Chemicals
Showing 20401–20550 of 41137 results
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GDC 0879 is an inhibitor of B-RafV600E (IC50 = 0.13 nM for human recombinant enzyme).{27943} It is selective for B-RafV600E over a panel of 140 kinases at a concentration of 1 μM. GDC 0879 inhibits phosphorylation of ERK in MALME-3M cells (IC50 = 63 nM) as well as phosphorylation of MEK1 in COLO 205 and A375 cells that express B-RafV600E (IC50s = 29 and 59 nM, respectively). In vivo, GDC 0879 (15-200 mg/kg) inhibits tumor growth in a dose-dependent manner in an A375 mouse xenograft model.
Brand:CaymanSKU:-Out of stock
GDC 0879 is an inhibitor of B-RafV600E (IC50 = 0.13 nM for human recombinant enzyme).{27943} It is selective for B-RafV600E over a panel of 140 kinases at a concentration of 1 μM. GDC 0879 inhibits phosphorylation of ERK in MALME-3M cells (IC50 = 63 nM) as well as phosphorylation of MEK1 in COLO 205 and A375 cells that express B-RafV600E (IC50s = 29 and 59 nM, respectively). In vivo, GDC 0879 (15-200 mg/kg) inhibits tumor growth in a dose-dependent manner in an A375 mouse xenograft model.
Brand:CaymanSKU:-Out of stock
GDC 0879 is an inhibitor of B-RafV600E (IC50 = 0.13 nM for human recombinant enzyme).{27943} It is selective for B-RafV600E over a panel of 140 kinases at a concentration of 1 μM. GDC 0879 inhibits phosphorylation of ERK in MALME-3M cells (IC50 = 63 nM) as well as phosphorylation of MEK1 in COLO 205 and A375 cells that express B-RafV600E (IC50s = 29 and 59 nM, respectively). In vivo, GDC 0879 (15-200 mg/kg) inhibits tumor growth in a dose-dependent manner in an A375 mouse xenograft model.
Brand:CaymanSKU:-Out of stock
GDC 0879 is an inhibitor of B-RafV600E (IC50 = 0.13 nM for human recombinant enzyme).{27943} It is selective for B-RafV600E over a panel of 140 kinases at a concentration of 1 μM. GDC 0879 inhibits phosphorylation of ERK in MALME-3M cells (IC50 = 63 nM) as well as phosphorylation of MEK1 in COLO 205 and A375 cells that express B-RafV600E (IC50s = 29 and 59 nM, respectively). In vivo, GDC 0879 (15-200 mg/kg) inhibits tumor growth in a dose-dependent manner in an A375 mouse xenograft model.
Brand:CaymanSKU:-Out of stock
GDC-0032 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K) isoforms α, δ, and γ (IC50s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ.{31881} It is over 1,000-fold selective for p100α over other PI3K-like kinases, including DNA-dependent protein kinase catalytic subunits, ATM, and ATR. GDC-0032 has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo, suppressing the growth of tumors in a mouse xenograft model at low drug dose levels.{31880,31881,31882}
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GDC-0032 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K) isoforms α, δ, and γ (IC50s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ.{31881} It is over 1,000-fold selective for p100α over other PI3K-like kinases, including DNA-dependent protein kinase catalytic subunits, ATM, and ATR. GDC-0032 has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo, suppressing the growth of tumors in a mouse xenograft model at low drug dose levels.{31880,31881,31882}
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GDC-0032 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K) isoforms α, δ, and γ (IC50s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ.{31881} It is over 1,000-fold selective for p100α over other PI3K-like kinases, including DNA-dependent protein kinase catalytic subunits, ATM, and ATR. GDC-0032 has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo, suppressing the growth of tumors in a mouse xenograft model at low drug dose levels.{31880,31881,31882}
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GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays.{30936} It is 620-fold selective for Akt over protein kinase A and has been shown to block Akt signaling selectively in cultured tumor cell lines characterized by activated Akt, halting cell cycle progression and reducing cell viability.{30936} In multiple tumor xenograft models, oral administration of GDC-0068 at 100 mg/kg/day can lead to delayed tumor growth and regression.{30936}
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GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays.{30936} It is 620-fold selective for Akt over protein kinase A and has been shown to block Akt signaling selectively in cultured tumor cell lines characterized by activated Akt, halting cell cycle progression and reducing cell viability.{30936} In multiple tumor xenograft models, oral administration of GDC-0068 at 100 mg/kg/day can lead to delayed tumor growth and regression.{30936}
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GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays.{30936} It is 620-fold selective for Akt over protein kinase A and has been shown to block Akt signaling selectively in cultured tumor cell lines characterized by activated Akt, halting cell cycle progression and reducing cell viability.{30936} In multiple tumor xenograft models, oral administration of GDC-0068 at 100 mg/kg/day can lead to delayed tumor growth and regression.{30936}
Brand:CaymanSKU:-Available on backorder
GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays.{30936} It is 620-fold selective for Akt over protein kinase A and has been shown to block Akt signaling selectively in cultured tumor cell lines characterized by activated Akt, halting cell cycle progression and reducing cell viability.{30936} In multiple tumor xenograft models, oral administration of GDC-0068 at 100 mg/kg/day can lead to delayed tumor growth and regression.{30936}
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GDC-0084 is a dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR) with Kiapp values of 2, 46, 3, 10, and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively.{45137} It inhibits the proliferation of PC3 cells in vitro (EC50 = 0.4 μM). GDC-0084 (25 mg/kg) reduces phosphorylation of Akt in mouse brain. It reduces tumor growth in a U87 MG/M human glioblastoma mouse xenograft model when administered at doses greater than 2.2 mg/kg and induces tumor regression when administered at a dose of 17.9 mg/kg. GDC-0084 (25 and 50 mg/kg) also reduces tumor growth in an A431 cutaneous squamous cell carcinoma (cSCC) mouse xenograft model.{45138}
Brand:CaymanSKU:26390 - 1 mgAvailable on backorder
GDC-0084 is a dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR) with Kiapp values of 2, 46, 3, 10, and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively.{45137} It inhibits the proliferation of PC3 cells in vitro (EC50 = 0.4 μM). GDC-0084 (25 mg/kg) reduces phosphorylation of Akt in mouse brain. It reduces tumor growth in a U87 MG/M human glioblastoma mouse xenograft model when administered at doses greater than 2.2 mg/kg and induces tumor regression when administered at a dose of 17.9 mg/kg. GDC-0084 (25 and 50 mg/kg) also reduces tumor growth in an A431 cutaneous squamous cell carcinoma (cSCC) mouse xenograft model.{45138}
Brand:CaymanSKU:26390 - 10 mgAvailable on backorder
GDC-0084 is a dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR) with Kiapp values of 2, 46, 3, 10, and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively.{45137} It inhibits the proliferation of PC3 cells in vitro (EC50 = 0.4 μM). GDC-0084 (25 mg/kg) reduces phosphorylation of Akt in mouse brain. It reduces tumor growth in a U87 MG/M human glioblastoma mouse xenograft model when administered at doses greater than 2.2 mg/kg and induces tumor regression when administered at a dose of 17.9 mg/kg. GDC-0084 (25 and 50 mg/kg) also reduces tumor growth in an A431 cutaneous squamous cell carcinoma (cSCC) mouse xenograft model.{45138}
Brand:CaymanSKU:26390 - 25 mgAvailable on backorder
GDC-0084 is a dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR) with Kiapp values of 2, 46, 3, 10, and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively.{45137} It inhibits the proliferation of PC3 cells in vitro (EC50 = 0.4 μM). GDC-0084 (25 mg/kg) reduces phosphorylation of Akt in mouse brain. It reduces tumor growth in a U87 MG/M human glioblastoma mouse xenograft model when administered at doses greater than 2.2 mg/kg and induces tumor regression when administered at a dose of 17.9 mg/kg. GDC-0084 (25 and 50 mg/kg) also reduces tumor growth in an A431 cutaneous squamous cell carcinoma (cSCC) mouse xenograft model.{45138}
Brand:CaymanSKU:26390 - 5 mgAvailable on backorder
Inhibitor of apoptosis proteins (IAPs), which block various signaling pathways leading to apoptotic cell death, are commonly over-expressed in cancer cells.{9448} GDC-0152 is a potent inhibitor of specific IAPs that binds baculoviral IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively).{29254} GDC-0152 induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.{29254,29255} It is orally bioavailable and suppresses tumor growth in breast cancer xenografts in mice.{29254} GDC-0152 also induces NF-κB transcriptional activity, resulting in the expression of several cytokines, including TNF-α.{29253} In dogs and rats, but not humans, this leads to a pronounced inflammatory response.{29253}
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Inhibitor of apoptosis proteins (IAPs), which block various signaling pathways leading to apoptotic cell death, are commonly over-expressed in cancer cells.{9448} GDC-0152 is a potent inhibitor of specific IAPs that binds baculoviral IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively).{29254} GDC-0152 induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.{29254,29255} It is orally bioavailable and suppresses tumor growth in breast cancer xenografts in mice.{29254} GDC-0152 also induces NF-κB transcriptional activity, resulting in the expression of several cytokines, including TNF-α.{29253} In dogs and rats, but not humans, this leads to a pronounced inflammatory response.{29253}
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Inhibitor of apoptosis proteins (IAPs), which block various signaling pathways leading to apoptotic cell death, are commonly over-expressed in cancer cells.{9448} GDC-0152 is a potent inhibitor of specific IAPs that binds baculoviral IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively).{29254} GDC-0152 induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.{29254,29255} It is orally bioavailable and suppresses tumor growth in breast cancer xenografts in mice.{29254} GDC-0152 also induces NF-κB transcriptional activity, resulting in the expression of several cytokines, including TNF-α.{29253} In dogs and rats, but not humans, this leads to a pronounced inflammatory response.{29253}
Brand:CaymanSKU:-Available on backorder
GDC-0326 is an inhibitor of phosphatidylinositol 3-kinase α (PI3Kα; Ki = 0.2 nM) that is 133-, 20-, and 51-fold selective for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively.{43203} It inhibits proliferation of MCF7-neo/HER2 and PC3 cells (EC50s = 0.1 and 2.2 μM, respectively). In vivo, GDC-0326 (6.25 mg/kg) induces tumor regression in a KPL-4 mouse xenograft model. It also reduces tumor growth, tumor vasculature, and the number of liver and lymph node metastases in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors.{43204}
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GDC-0326 is an inhibitor of phosphatidylinositol 3-kinase α (PI3Kα; Ki = 0.2 nM) that is 133-, 20-, and 51-fold selective for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively.{43203} It inhibits proliferation of MCF7-neo/HER2 and PC3 cells (EC50s = 0.1 and 2.2 μM, respectively). In vivo, GDC-0326 (6.25 mg/kg) induces tumor regression in a KPL-4 mouse xenograft model. It also reduces tumor growth, tumor vasculature, and the number of liver and lymph node metastases in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors.{43204}
Brand:CaymanSKU:-Available on backorder
GDC-0326 is an inhibitor of phosphatidylinositol 3-kinase α (PI3Kα; Ki = 0.2 nM) that is 133-, 20-, and 51-fold selective for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively.{43203} It inhibits proliferation of MCF7-neo/HER2 and PC3 cells (EC50s = 0.1 and 2.2 μM, respectively). In vivo, GDC-0326 (6.25 mg/kg) induces tumor regression in a KPL-4 mouse xenograft model. It also reduces tumor growth, tumor vasculature, and the number of liver and lymph node metastases in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors.{43204}
Brand:CaymanSKU:-Available on backorder
GDC-0326 is an inhibitor of phosphatidylinositol 3-kinase α (PI3Kα; Ki = 0.2 nM) that is 133-, 20-, and 51-fold selective for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively.{43203} It inhibits proliferation of MCF7-neo/HER2 and PC3 cells (EC50s = 0.1 and 2.2 μM, respectively). In vivo, GDC-0326 (6.25 mg/kg) induces tumor regression in a KPL-4 mouse xenograft model. It also reduces tumor growth, tumor vasculature, and the number of liver and lymph node metastases in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors.{43204}
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GDC-0349 is a potent inhibitor of the mammalian target of rapamycin (mTOR; Ki = 3.8 nM).{41444} It is selective for mTOR over a panel of 266 kinases at a concentration of 1 μM. GDC-0349 inhibits proliferation of PC3 prostate cancer cells in vitro (EC50 = 270 nM) and induces caspase-dependent apoptosis in head and neck squamous cell carcinoma (HNSCC) cells via inhibition of mTOR complex 1 (mTORC1) and mTORC2 and induction of autophagy.{41444,41445} Oral administration of GDC-0349 (10-80 mg/kg) inhibits tumor growth in MCF7-neo/Her-2 breast and PC3 prostate cancer mouse xenograft models in a dose-dependent manner. It also reduces tumor growth in an A549 lung cancer mouse xenograft model when administered in combination with the PI3K inhibitor GDC-0941 (Item No. 11600) or the MEK inhibitor cobimetinib (GDC-0973; Item No. 19563).
Brand:CaymanSKU:24058 - 1 mgAvailable on backorder
GDC-0349 is a potent inhibitor of the mammalian target of rapamycin (mTOR; Ki = 3.8 nM).{41444} It is selective for mTOR over a panel of 266 kinases at a concentration of 1 μM. GDC-0349 inhibits proliferation of PC3 prostate cancer cells in vitro (EC50 = 270 nM) and induces caspase-dependent apoptosis in head and neck squamous cell carcinoma (HNSCC) cells via inhibition of mTOR complex 1 (mTORC1) and mTORC2 and induction of autophagy.{41444,41445} Oral administration of GDC-0349 (10-80 mg/kg) inhibits tumor growth in MCF7-neo/Her-2 breast and PC3 prostate cancer mouse xenograft models in a dose-dependent manner. It also reduces tumor growth in an A549 lung cancer mouse xenograft model when administered in combination with the PI3K inhibitor GDC-0941 (Item No. 11600) or the MEK inhibitor cobimetinib (GDC-0973; Item No. 19563).
Brand:CaymanSKU:24058 - 10 mgAvailable on backorder
GDC-0349 is a potent inhibitor of the mammalian target of rapamycin (mTOR; Ki = 3.8 nM).{41444} It is selective for mTOR over a panel of 266 kinases at a concentration of 1 μM. GDC-0349 inhibits proliferation of PC3 prostate cancer cells in vitro (EC50 = 270 nM) and induces caspase-dependent apoptosis in head and neck squamous cell carcinoma (HNSCC) cells via inhibition of mTOR complex 1 (mTORC1) and mTORC2 and induction of autophagy.{41444,41445} Oral administration of GDC-0349 (10-80 mg/kg) inhibits tumor growth in MCF7-neo/Her-2 breast and PC3 prostate cancer mouse xenograft models in a dose-dependent manner. It also reduces tumor growth in an A549 lung cancer mouse xenograft model when administered in combination with the PI3K inhibitor GDC-0941 (Item No. 11600) or the MEK inhibitor cobimetinib (GDC-0973; Item No. 19563).
Brand:CaymanSKU:24058 - 5 mgAvailable on backorder
GDC-0349 is a potent inhibitor of the mammalian target of rapamycin (mTOR; Ki = 3.8 nM).{41444} It is selective for mTOR over a panel of 266 kinases at a concentration of 1 μM. GDC-0349 inhibits proliferation of PC3 prostate cancer cells in vitro (EC50 = 270 nM) and induces caspase-dependent apoptosis in head and neck squamous cell carcinoma (HNSCC) cells via inhibition of mTOR complex 1 (mTORC1) and mTORC2 and induction of autophagy.{41444,41445} Oral administration of GDC-0349 (10-80 mg/kg) inhibits tumor growth in MCF7-neo/Her-2 breast and PC3 prostate cancer mouse xenograft models in a dose-dependent manner. It also reduces tumor growth in an A549 lung cancer mouse xenograft model when administered in combination with the PI3K inhibitor GDC-0941 (Item No. 11600) or the MEK inhibitor cobimetinib (GDC-0973; Item No. 19563).
Brand:CaymanSKU:24058 - 500 µgAvailable on backorder
GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki = 0.13 nM in the presence of ATP).{33319} It inhibits the proliferation of A375 BRAF(V600E) and HCT116 KRAS(G13D)-mutant cancer cell lines with EC50 values of 7 and 42 nM, respectively.{33319} GDC-0623 inhibits ERK and BIM phosphorylation resulting in upregulation and stabilization of pro-apoptotic BIM protein in KRAS mutant and wild-type HCT116 cells and in KRAS mutant GW620 cells.{33320}
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GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki = 0.13 nM in the presence of ATP).{33319} It inhibits the proliferation of A375 BRAF(V600E) and HCT116 KRAS(G13D)-mutant cancer cell lines with EC50 values of 7 and 42 nM, respectively.{33319} GDC-0623 inhibits ERK and BIM phosphorylation resulting in upregulation and stabilization of pro-apoptotic BIM protein in KRAS mutant and wild-type HCT116 cells and in KRAS mutant GW620 cells.{33320}
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GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki = 0.13 nM in the presence of ATP).{33319} It inhibits the proliferation of A375 BRAF(V600E) and HCT116 KRAS(G13D)-mutant cancer cell lines with EC50 values of 7 and 42 nM, respectively.{33319} GDC-0623 inhibits ERK and BIM phosphorylation resulting in upregulation and stabilization of pro-apoptotic BIM protein in KRAS mutant and wild-type HCT116 cells and in KRAS mutant GW620 cells.{33320}
Brand:CaymanSKU:-Available on backorder
GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki = 0.13 nM in the presence of ATP).{33319} It inhibits the proliferation of A375 BRAF(V600E) and HCT116 KRAS(G13D)-mutant cancer cell lines with EC50 values of 7 and 42 nM, respectively.{33319} GDC-0623 inhibits ERK and BIM phosphorylation resulting in upregulation and stabilization of pro-apoptotic BIM protein in KRAS mutant and wild-type HCT116 cells and in KRAS mutant GW620 cells.{33320}
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GDC-0853 is an orally bioavailable, selective, and reversible Bruton’s tyrosine kinase (BTK) inhibitor with IC50s ranging from 2-9 nM for basophil activation, B cell receptor activation, and constitutive p-BTK activity in whole blood lysates.{34260,34261} In rats, treatment for longer than 7 days leads to pancreatic toxicity but it does not occur in mice or dogs, even at higher doses.{34259} Formulations containing GDC-0853 were well-tolerated in Phase I clinical trials and are in additional clinical trials for rheumatoid arthritis, lupus erythematosus, lymphoma, and leukemia.
Brand:CaymanSKU:21346 -Out of stock
GDC-0853 is an orally bioavailable, selective, and reversible Bruton’s tyrosine kinase (BTK) inhibitor with IC50s ranging from 2-9 nM for basophil activation, B cell receptor activation, and constitutive p-BTK activity in whole blood lysates.{34260,34261} In rats, treatment for longer than 7 days leads to pancreatic toxicity but it does not occur in mice or dogs, even at higher doses.{34259} Formulations containing GDC-0853 were well-tolerated in Phase I clinical trials and are in additional clinical trials for rheumatoid arthritis, lupus erythematosus, lymphoma, and leukemia.
Brand:CaymanSKU:21346 -Out of stock
GDC-0853 is an orally bioavailable, selective, and reversible Bruton’s tyrosine kinase (BTK) inhibitor with IC50s ranging from 2-9 nM for basophil activation, B cell receptor activation, and constitutive p-BTK activity in whole blood lysates.{34260,34261} In rats, treatment for longer than 7 days leads to pancreatic toxicity but it does not occur in mice or dogs, even at higher doses.{34259} Formulations containing GDC-0853 were well-tolerated in Phase I clinical trials and are in additional clinical trials for rheumatoid arthritis, lupus erythematosus, lymphoma, and leukemia.
Brand:CaymanSKU:21346 -Out of stock
GDC-0853 is an orally bioavailable, selective, and reversible Bruton’s tyrosine kinase (BTK) inhibitor with IC50s ranging from 2-9 nM for basophil activation, B cell receptor activation, and constitutive p-BTK activity in whole blood lysates.{34260,34261} In rats, treatment for longer than 7 days leads to pancreatic toxicity but it does not occur in mice or dogs, even at higher doses.{34259} Formulations containing GDC-0853 were well-tolerated in Phase I clinical trials and are in additional clinical trials for rheumatoid arthritis, lupus erythematosus, lymphoma, and leukemia.
Brand:CaymanSKU:21346 -Out of stock
The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival.{13740,17822} GDC-0941 is a potent pan inhibitor of class I catalytic subunits of PI3K, inhibiting p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively.{24602,24604} It is much less effective against class II-IV isoforms of PI3K and against mTOR.{24602,24603} GDC-0941 inhibits the growth of certain types of cancer cells and blocks signaling through PI3K to Akt, both in cells and in vivo.{24602,24605}
Brand:CaymanSKU:11600 - 10 mgAvailable on backorder
The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival.{13740,17822} GDC-0941 is a potent pan inhibitor of class I catalytic subunits of PI3K, inhibiting p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively.{24602,24604} It is much less effective against class II-IV isoforms of PI3K and against mTOR.{24602,24603} GDC-0941 inhibits the growth of certain types of cancer cells and blocks signaling through PI3K to Akt, both in cells and in vivo.{24602,24605}
Brand:CaymanSKU:11600 - 100 mgAvailable on backorder
The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival.{13740,17822} GDC-0941 is a potent pan inhibitor of class I catalytic subunits of PI3K, inhibiting p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively.{24602,24604} It is much less effective against class II-IV isoforms of PI3K and against mTOR.{24602,24603} GDC-0941 inhibits the growth of certain types of cancer cells and blocks signaling through PI3K to Akt, both in cells and in vivo.{24602,24605}
Brand:CaymanSKU:11600 - 50 mgAvailable on backorder
GDC-0980 is a potent inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms, with IC50 values of 5, 27, 7, and 14 nM for PI3Kα, β, δ, and γ, respectively, in cell-free assays.{29877,29878} It also inhibits mTOR (Ki = 17 nM) but is inactive against a large panel of additional kinases.{29877,29878} GDC-0980 induces cell cycle arrest or apoptosis in a range of cancer cell lines.{29878} It is effective in vivo, suppressing the growth of a number of tumor xenografts in mice and enhancing the antitumor activity of docetaxel (Item No. 11637) in mice.{29878}
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GDC-0980 is a potent inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms, with IC50 values of 5, 27, 7, and 14 nM for PI3Kα, β, δ, and γ, respectively, in cell-free assays.{29877,29878} It also inhibits mTOR (Ki = 17 nM) but is inactive against a large panel of additional kinases.{29877,29878} GDC-0980 induces cell cycle arrest or apoptosis in a range of cancer cell lines.{29878} It is effective in vivo, suppressing the growth of a number of tumor xenografts in mice and enhancing the antitumor activity of docetaxel (Item No. 11637) in mice.{29878}
Brand:CaymanSKU:-Available on backorder
GDC-0980 is a potent inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms, with IC50 values of 5, 27, 7, and 14 nM for PI3Kα, β, δ, and γ, respectively, in cell-free assays.{29877,29878} It also inhibits mTOR (Ki = 17 nM) but is inactive against a large panel of additional kinases.{29877,29878} GDC-0980 induces cell cycle arrest or apoptosis in a range of cancer cell lines.{29878} It is effective in vivo, suppressing the growth of a number of tumor xenografts in mice and enhancing the antitumor activity of docetaxel (Item No. 11637) in mice.{29878}
Brand:CaymanSKU:-Available on backorder
GDC-0980 is a potent inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms, with IC50 values of 5, 27, 7, and 14 nM for PI3Kα, β, δ, and γ, respectively, in cell-free assays.{29877,29878} It also inhibits mTOR (Ki = 17 nM) but is inactive against a large panel of additional kinases.{29877,29878} GDC-0980 induces cell cycle arrest or apoptosis in a range of cancer cell lines.{29878} It is effective in vivo, suppressing the growth of a number of tumor xenografts in mice and enhancing the antitumor activity of docetaxel (Item No. 11637) in mice.{29878}
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GDC-0994 is a potent and selective ERK1 and ERK2 inhibitor with IC50 values of 6.1 and 4.1 nM, respectively.{33248} It inhibits ERK-dependent p90RSK serine 380 phosphorylation in PMA-stimulated HepG2 cells with an IC50 value of 12 nM. GDC-0994 inhibited growth of HCT116 human colorectal cancer xenograft tumors by 49%, 57%, and 80% at 30, 60, and 100 mg/kg, respectively, when administered orally once daily for 21 days.{33248}
Brand:CaymanSKU:21107 -Out of stock
GDC-0994 is a potent and selective ERK1 and ERK2 inhibitor with IC50 values of 6.1 and 4.1 nM, respectively.{33248} It inhibits ERK-dependent p90RSK serine 380 phosphorylation in PMA-stimulated HepG2 cells with an IC50 value of 12 nM. GDC-0994 inhibited growth of HCT116 human colorectal cancer xenograft tumors by 49%, 57%, and 80% at 30, 60, and 100 mg/kg, respectively, when administered orally once daily for 21 days.{33248}
Brand:CaymanSKU:21107 -Out of stock
GDC-0994 is a potent and selective ERK1 and ERK2 inhibitor with IC50 values of 6.1 and 4.1 nM, respectively.{33248} It inhibits ERK-dependent p90RSK serine 380 phosphorylation in PMA-stimulated HepG2 cells with an IC50 value of 12 nM. GDC-0994 inhibited growth of HCT116 human colorectal cancer xenograft tumors by 49%, 57%, and 80% at 30, 60, and 100 mg/kg, respectively, when administered orally once daily for 21 days.{33248}
Brand:CaymanSKU:21107 -Out of stock
GDC-0994 is a potent and selective ERK1 and ERK2 inhibitor with IC50 values of 6.1 and 4.1 nM, respectively.{33248} It inhibits ERK-dependent p90RSK serine 380 phosphorylation in PMA-stimulated HepG2 cells with an IC50 value of 12 nM. GDC-0994 inhibited growth of HCT116 human colorectal cancer xenograft tumors by 49%, 57%, and 80% at 30, 60, and 100 mg/kg, respectively, when administered orally once daily for 21 days.{33248}
Brand:CaymanSKU:21107 -Out of stock
Gedunin is a natural inhibitor of the heat shock protein (Hsp90; Item Nos. 22734 | 22735) co-chaperone p23 that also inhibits Hsp90 expression in human teratocarcinomal NTERA-2 cells in vitro at 5 µg/ml.{35153} This tetranortriterpenoid, which is isolated from A. indica, binds to and blocks the chaperone activity of p23 to induce apoptosis in HeLa-PRB cells in vitro at a concentration of 20 µM.{35151} Gedunin inhibits breast cancer cell proliferation in vitro, with IC50 values of 8.84 and 3.22 µM in MCF-7 and SKBr-3 cells, respectively, and inhibits the growth of PANC-1 pancreatic cancer cells (IC50 = 25 µM) by targeting the sonic hedgehog pathway to induce apoptosis.{35147,35152} It also exerts anti-inflammatory effects in vivo. In a mouse model of articular inflammation induced by zymosan (Item No. 21175), gedunin (0.05-0.5 mg/kg, i.p.) reduces edema formation and the production of inflammatory cytokines.{35149} Gedunin (0.5 mg/kg) also inhibits the pleural accumulation of eosinophils and activated T lymphocytes in an ovalbumin-sensitized mouse model of allergic inflammation when administered prior to ovalbumin rechallenge.{35150} It also targets the lipopolysaccharide binding site and thus blocks Toll-like receptor 4 (TLR4) signaling in macrophages in vitro at a concentration of 10 µM.{35145}
Brand:CaymanSKU:-Available on backorder
Gefitinib is a selective EGFR-TK inhibitor that blocks the growth of GEO colon, ZR-75-1, and MCF-10A Ha-ras breast, and OVCAR-3 ovarian cancer cell lines with IC50 values of 0.2-0.4 µM.{17856} By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Formulations containing gefitinib were previously used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval when a phase III trial failed to demonstrate an overall survival benefit.{17857} Formulations containing gefitinib appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations.{17858,17859}
Brand:CaymanSKU:- Gefitinib is a selective EGFR-TK inhibitor that blocks the growth of GEO colon, ZR-75-1, and MCF-10A Ha-ras breast, and OVCAR-3 ovarian cancer cell lines with IC50 values of 0.2-0.4 µM.{17856} By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Formulations containing gefitinib were previously used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval when a phase III trial failed to demonstrate an overall survival benefit.{17857} Formulations containing gefitinib appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations.{17858,17859}
Brand:CaymanSKU:- Gefitinib is a selective EGFR-TK inhibitor that blocks the growth of GEO colon, ZR-75-1, and MCF-10A Ha-ras breast, and OVCAR-3 ovarian cancer cell lines with IC50 values of 0.2-0.4 µM.{17856} By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Formulations containing gefitinib were previously used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval when a phase III trial failed to demonstrate an overall survival benefit.{17857} Formulations containing gefitinib appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations.{17858,17859}
Brand:CaymanSKU:- Gefitinib is a selective EGFR-TK inhibitor that blocks the growth of GEO colon, ZR-75-1, and MCF-10A Ha-ras breast, and OVCAR-3 ovarian cancer cell lines with IC50 values of 0.2-0.4 µM.{17856} By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Formulations containing gefitinib were previously used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval when a phase III trial failed to demonstrate an overall survival benefit.{17857} Formulations containing gefitinib appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations.{17858,17859}
Brand:CaymanSKU:-
Gefitinib-based PROTAC 3 is a proteolysis-targeting chimera (PROTAC) comprised of the EGF receptor (EGFR) inhibitor gefitinib (Item No. 13166) linked to the von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand VHL ligand 1 (Item No. 21591).{52051} In cell-based assays, gefitinib-based PROTAC 3 induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion with half-maximal degradation (DC50) values of 22.3 and 11.7 nM, respectively, but does not induce degradation of wild-type EGFR at concentrations up to 10 μM.
Brand:CaymanSKU:28597 - 1 mgAvailable on backorder
Gefitinib-based PROTAC 3 is a proteolysis-targeting chimera (PROTAC) comprised of the EGF receptor (EGFR) inhibitor gefitinib (Item No. 13166) linked to the von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand VHL ligand 1 (Item No. 21591).{52051} In cell-based assays, gefitinib-based PROTAC 3 induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion with half-maximal degradation (DC50) values of 22.3 and 11.7 nM, respectively, but does not induce degradation of wild-type EGFR at concentrations up to 10 μM.
Brand:CaymanSKU:28597 - 10 mgAvailable on backorder
Gefitinib-based PROTAC 3 is a proteolysis-targeting chimera (PROTAC) comprised of the EGF receptor (EGFR) inhibitor gefitinib (Item No. 13166) linked to the von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand VHL ligand 1 (Item No. 21591).{52051} In cell-based assays, gefitinib-based PROTAC 3 induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion with half-maximal degradation (DC50) values of 22.3 and 11.7 nM, respectively, but does not induce degradation of wild-type EGFR at concentrations up to 10 μM.
Brand:CaymanSKU:28597 - 25 mgAvailable on backorder
Gefitinib-based PROTAC 3 is a proteolysis-targeting chimera (PROTAC) comprised of the EGF receptor (EGFR) inhibitor gefitinib (Item No. 13166) linked to the von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand VHL ligand 1 (Item No. 21591).{52051} In cell-based assays, gefitinib-based PROTAC 3 induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion with half-maximal degradation (DC50) values of 22.3 and 11.7 nM, respectively, but does not induce degradation of wild-type EGFR at concentrations up to 10 μM.
Brand:CaymanSKU:28597 - 5 mgAvailable on backorder
Gefitinib-d6 is intended for use as an internal standard for the quantification of gefitinib (Item No. 13166) by GC- or LC-MS. Gefitinib is a selective EGFR-TK inhibitor that blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50s ranging between 0.2-0.4 µM.{17856} By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Formulations containing gefitinib were previously used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval when a phase III trial failed to demonstrate an overall survival benefit.{17857} Formulations containing gefitinib appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations.{17858,17859}
Brand:CaymanSKU:22364 -Out of stock
Gefitinib-d6 is intended for use as an internal standard for the quantification of gefitinib (Item No. 13166) by GC- or LC-MS. Gefitinib is a selective EGFR-TK inhibitor that blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50s ranging between 0.2-0.4 µM.{17856} By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Formulations containing gefitinib were previously used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval when a phase III trial failed to demonstrate an overall survival benefit.{17857} Formulations containing gefitinib appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations.{17858,17859}
Brand:CaymanSKU:22364 -Out of stock
Geldanamycin is a benzoquinone ansamycin antibiotic which binds heat shock protein 90 (Hsp90) and its paralog GRP94, altering their actions.{15573,18242,18246} Through its interaction with these chaperones, geldanamycin indirectly affects numerous client proteins with roles in diverse cellular processes, including gene expression, cell proliferation, apoptosis, and angiogenesis. For example, geldanamycin inhibits c-jun expression in human colon adenocarcinoma HT29 cells (IC50 = 75 nM), inhibiting AP-1 binding.{18245} It also reduces signaling through mitogenic signaling proteins and interferes with steroid receptor function.{15573,18247,18243,18244} Inhibitors of Hsp90, including geldanamycin, show promise in cancer therapy.{18248}
Brand:CaymanSKU:- Geldanamycin is a benzoquinone ansamycin antibiotic which binds heat shock protein 90 (Hsp90) and its paralog GRP94, altering their actions.{15573,18242,18246} Through its interaction with these chaperones, geldanamycin indirectly affects numerous client proteins with roles in diverse cellular processes, including gene expression, cell proliferation, apoptosis, and angiogenesis. For example, geldanamycin inhibits c-jun expression in human colon adenocarcinoma HT29 cells (IC50 = 75 nM), inhibiting AP-1 binding.{18245} It also reduces signaling through mitogenic signaling proteins and interferes with steroid receptor function.{15573,18247,18243,18244} Inhibitors of Hsp90, including geldanamycin, show promise in cancer therapy.{18248}
Brand:CaymanSKU:- Geldanamycin is a benzoquinone ansamycin antibiotic which binds heat shock protein 90 (Hsp90) and its paralog GRP94, altering their actions.{15573,18242,18246} Through its interaction with these chaperones, geldanamycin indirectly affects numerous client proteins with roles in diverse cellular processes, including gene expression, cell proliferation, apoptosis, and angiogenesis. For example, geldanamycin inhibits c-jun expression in human colon adenocarcinoma HT29 cells (IC50 = 75 nM), inhibiting AP-1 binding.{18245} It also reduces signaling through mitogenic signaling proteins and interferes with steroid receptor function.{15573,18247,18243,18244} Inhibitors of Hsp90, including geldanamycin, show promise in cancer therapy.{18248}
Brand:CaymanSKU:-
Gemcitabine is an anticancer nucleoside analog that inhibits the growth of HL-60 promyelocytic leukemia cells with an LC50 value of 40 nM.{40344} It inhibits the growth of MX-1 mammary, CX-1, HC-1, GC3, and VRC5 colon, LX-1, Calu-6, and NCI-H460 lung, and HS766T, PaCa-2, PANC-1, and BxPC-3 pancreatic cancer tumors in mouse xenograft models (45-93% inhibition).{40343} Gemcitabine is a prodrug that is metabolized to a diphosphate and triphosphate form in cells. The triphosphate form is incorporated into DNA which induces masked chain termination and cell death.{21021} By specifically inhibiting growth arrest and DNA damage inducible protein 45 a (Gadd45a), a key mediator of active DNA demethylation, gemcitabine, at concentrations ranging from 34 to 134 nM, inhibits repair-mediated DNA demethylation in a methylation-sensitive reporter assay. Gemcitabine also has broad antiretroviral activity, decreasing MuLV cell infectivity, a murine AIDS model, in cell culture (EC50 = ~1.5 nM) and inhibits the progression of murine AIDS in vivo at a dose of 1-2 mg/kg per day.{21022}
Brand:CaymanSKU:11690 - 10 mgAvailable on backorder
Gemcitabine is an anticancer nucleoside analog that inhibits the growth of HL-60 promyelocytic leukemia cells with an LC50 value of 40 nM.{40344} It inhibits the growth of MX-1 mammary, CX-1, HC-1, GC3, and VRC5 colon, LX-1, Calu-6, and NCI-H460 lung, and HS766T, PaCa-2, PANC-1, and BxPC-3 pancreatic cancer tumors in mouse xenograft models (45-93% inhibition).{40343} Gemcitabine is a prodrug that is metabolized to a diphosphate and triphosphate form in cells. The triphosphate form is incorporated into DNA which induces masked chain termination and cell death.{21021} By specifically inhibiting growth arrest and DNA damage inducible protein 45 a (Gadd45a), a key mediator of active DNA demethylation, gemcitabine, at concentrations ranging from 34 to 134 nM, inhibits repair-mediated DNA demethylation in a methylation-sensitive reporter assay. Gemcitabine also has broad antiretroviral activity, decreasing MuLV cell infectivity, a murine AIDS model, in cell culture (EC50 = ~1.5 nM) and inhibits the progression of murine AIDS in vivo at a dose of 1-2 mg/kg per day.{21022}
Brand:CaymanSKU:11690 - 100 mgAvailable on backorder
Gemcitabine is an anticancer nucleoside analog that inhibits the growth of HL-60 promyelocytic leukemia cells with an LC50 value of 40 nM.{40344} It inhibits the growth of MX-1 mammary, CX-1, HC-1, GC3, and VRC5 colon, LX-1, Calu-6, and NCI-H460 lung, and HS766T, PaCa-2, PANC-1, and BxPC-3 pancreatic cancer tumors in mouse xenograft models (45-93% inhibition).{40343} Gemcitabine is a prodrug that is metabolized to a diphosphate and triphosphate form in cells. The triphosphate form is incorporated into DNA which induces masked chain termination and cell death.{21021} By specifically inhibiting growth arrest and DNA damage inducible protein 45 a (Gadd45a), a key mediator of active DNA demethylation, gemcitabine, at concentrations ranging from 34 to 134 nM, inhibits repair-mediated DNA demethylation in a methylation-sensitive reporter assay. Gemcitabine also has broad antiretroviral activity, decreasing MuLV cell infectivity, a murine AIDS model, in cell culture (EC50 = ~1.5 nM) and inhibits the progression of murine AIDS in vivo at a dose of 1-2 mg/kg per day.{21022}
Brand:CaymanSKU:11690 - 25 mgAvailable on backorder
Gemcitabine is an anticancer nucleoside analog that inhibits the growth of HL-60 promyelocytic leukemia cells with an LC50 value of 40 nM.{40344} It inhibits the growth of MX-1 mammary, CX-1, HC-1, GC3, and VRC5 colon, LX-1, Calu-6, and NCI-H460 lung, and HS766T, PaCa-2, PANC-1, and BxPC-3 pancreatic cancer tumors in mouse xenograft models (45-93% inhibition).{40343} Gemcitabine is a prodrug that is metabolized to a diphosphate and triphosphate form in cells. The triphosphate form is incorporated into DNA which induces masked chain termination and cell death.{21021} By specifically inhibiting growth arrest and DNA damage inducible protein 45 a (Gadd45a), a key mediator of active DNA demethylation, gemcitabine, at concentrations ranging from 34 to 134 nM, inhibits repair-mediated DNA demethylation in a methylation-sensitive reporter assay. Gemcitabine also has broad antiretroviral activity, decreasing MuLV cell infectivity, a murine AIDS model, in cell culture (EC50 = ~1.5 nM) and inhibits the progression of murine AIDS in vivo at a dose of 1-2 mg/kg per day.{21022}
Brand:CaymanSKU:11690 - 50 mgAvailable on backorder
Gemcitabine is an anticancer nucleoside analog that inhibits the growth of HL-60 promyelocytic leukemia cells with an LC50 value of 40 nM.{40344} It inhibits the growth of MX-1 mammary, CX-1, HC-1, GC3, and VRC5 colon, LX-1, Calu-6, and NCI-H460 lung, and HS766T, PaCa-2, PANC-1, and BxPC-3 pancreatic cancer tumors in mouse xenograft models (45-93% inhibition).{40343} Gemcitabine is a prodrug that is metabolized to a diphosphate and triphosphate form in cells. The triphosphate form is incorporated into DNA which induces masked chain termination and cell death.{21021} By specifically inhibiting growth arrest and DNA damage inducible protein 45 a (Gadd45a), a key mediator of active DNA demethylation, gemcitabine, at concentrations ranging from 34 to 134 nM, inhibits repair-mediated DNA demethylation in a methylation-sensitive reporter assay. Gemcitabine also has broad antiretroviral activity, decreasing MuLV cell infectivity, a murine AIDS model, in cell culture (EC50 = ~1.5 nM) and inhibits the progression of murine AIDS in vivo at a dose of 1-2 mg/kg per day.{21022}
Brand:CaymanSKU:9003096 - 100 mgAvailable on backorder
Gemcitabine is an anticancer nucleoside analog that inhibits the growth of HL-60 promyelocytic leukemia cells with an LC50 value of 40 nM.{40344} It inhibits the growth of MX-1 mammary, CX-1, HC-1, GC3, and VRC5 colon, LX-1, Calu-6, and NCI-H460 lung, and HS766T, PaCa-2, PANC-1, and BxPC-3 pancreatic cancer tumors in mouse xenograft models (45-93% inhibition).{40343} Gemcitabine is a prodrug that is metabolized to a diphosphate and triphosphate form in cells. The triphosphate form is incorporated into DNA which induces masked chain termination and cell death.{21021} By specifically inhibiting growth arrest and DNA damage inducible protein 45 a (Gadd45a), a key mediator of active DNA demethylation, gemcitabine, at concentrations ranging from 34 to 134 nM, inhibits repair-mediated DNA demethylation in a methylation-sensitive reporter assay. Gemcitabine also has broad antiretroviral activity, decreasing MuLV cell infectivity, a murine AIDS model, in cell culture (EC50 = ~1.5 nM) and inhibits the progression of murine AIDS in vivo at a dose of 1-2 mg/kg per day.{21022}
Brand:CaymanSKU:9003096 - 25 mgAvailable on backorder
Gemcitabine is an anticancer nucleoside analog that inhibits the growth of HL-60 promyelocytic leukemia cells with an LC50 value of 40 nM.{40344} It inhibits the growth of MX-1 mammary, CX-1, HC-1, GC3, and VRC5 colon, LX-1, Calu-6, and NCI-H460 lung, and HS766T, PaCa-2, PANC-1, and BxPC-3 pancreatic cancer tumors in mouse xenograft models (45-93% inhibition).{40343} Gemcitabine is a prodrug that is metabolized to a diphosphate and triphosphate form in cells. The triphosphate form is incorporated into DNA which induces masked chain termination and cell death.{21021} By specifically inhibiting growth arrest and DNA damage inducible protein 45 a (Gadd45a), a key mediator of active DNA demethylation, gemcitabine, at concentrations ranging from 34 to 134 nM, inhibits repair-mediated DNA demethylation in a methylation-sensitive reporter assay. Gemcitabine also has broad antiretroviral activity, decreasing MuLV cell infectivity, a murine AIDS model, in cell culture (EC50 = ~1.5 nM) and inhibits the progression of murine AIDS in vivo at a dose of 1-2 mg/kg per day.{21022}
Brand:CaymanSKU:9003096 - 50 mgAvailable on backorder
Gemcitabine elaidate is a lipophilic prodrug form of the nucleoside analog gemcitabine (Item Nos. 11690 | 9003096) that contains an elaidic acid (Item No. 90250) moiety.{47590} Gemcitabine elaidate inhibits growth of gemcitabine-sensitive L1210/L5, BCLO, and A2780 cells (IC50s = 0.0033, 0.0042, and 0.0025 µM, respectively) but not cytarabine-resistant L4A6 and Bara-C cells (IC50s = 16 and 13 µM, respectively) or gemcitabine-resistant AG6000 cells (IC50 = 91 µM). It inhibits growth of THX, LOX, MOLT-4, and MOLT-4/C8 cells in a manner independent of nucleoside transport. Gemcitabine elaidate reduces tumor growth in EKVX non-small cell lung cancer and MHMX sarcoma mouse xenograft models but not in an H-146 small cell lung cancer mouse xenograft model when administered at a dose of 40 mg/kg every three days.
Brand:CaymanSKU:28303 - 1 mgAvailable on backorder
Gemcitabine elaidate is a lipophilic prodrug form of the nucleoside analog gemcitabine (Item Nos. 11690 | 9003096) that contains an elaidic acid (Item No. 90250) moiety.{47590} Gemcitabine elaidate inhibits growth of gemcitabine-sensitive L1210/L5, BCLO, and A2780 cells (IC50s = 0.0033, 0.0042, and 0.0025 µM, respectively) but not cytarabine-resistant L4A6 and Bara-C cells (IC50s = 16 and 13 µM, respectively) or gemcitabine-resistant AG6000 cells (IC50 = 91 µM). It inhibits growth of THX, LOX, MOLT-4, and MOLT-4/C8 cells in a manner independent of nucleoside transport. Gemcitabine elaidate reduces tumor growth in EKVX non-small cell lung cancer and MHMX sarcoma mouse xenograft models but not in an H-146 small cell lung cancer mouse xenograft model when administered at a dose of 40 mg/kg every three days.
Brand:CaymanSKU:28303 - 10 mgAvailable on backorder
Gemcitabine elaidate is a lipophilic prodrug form of the nucleoside analog gemcitabine (Item Nos. 11690 | 9003096) that contains an elaidic acid (Item No. 90250) moiety.{47590} Gemcitabine elaidate inhibits growth of gemcitabine-sensitive L1210/L5, BCLO, and A2780 cells (IC50s = 0.0033, 0.0042, and 0.0025 µM, respectively) but not cytarabine-resistant L4A6 and Bara-C cells (IC50s = 16 and 13 µM, respectively) or gemcitabine-resistant AG6000 cells (IC50 = 91 µM). It inhibits growth of THX, LOX, MOLT-4, and MOLT-4/C8 cells in a manner independent of nucleoside transport. Gemcitabine elaidate reduces tumor growth in EKVX non-small cell lung cancer and MHMX sarcoma mouse xenograft models but not in an H-146 small cell lung cancer mouse xenograft model when administered at a dose of 40 mg/kg every three days.
Brand:CaymanSKU:28303 - 25 mgAvailable on backorder
Gemcitabine elaidate is a lipophilic prodrug form of the nucleoside analog gemcitabine (Item Nos. 11690 | 9003096) that contains an elaidic acid (Item No. 90250) moiety.{47590} Gemcitabine elaidate inhibits growth of gemcitabine-sensitive L1210/L5, BCLO, and A2780 cells (IC50s = 0.0033, 0.0042, and 0.0025 µM, respectively) but not cytarabine-resistant L4A6 and Bara-C cells (IC50s = 16 and 13 µM, respectively) or gemcitabine-resistant AG6000 cells (IC50 = 91 µM). It inhibits growth of THX, LOX, MOLT-4, and MOLT-4/C8 cells in a manner independent of nucleoside transport. Gemcitabine elaidate reduces tumor growth in EKVX non-small cell lung cancer and MHMX sarcoma mouse xenograft models but not in an H-146 small cell lung cancer mouse xenograft model when administered at a dose of 40 mg/kg every three days.
Brand:CaymanSKU:28303 - 5 mgAvailable on backorder
Gemcitabine monophosphate is a monophosphate form of the deoxycytidine analog gemcitabine (Item No. 9003096).{40694} It has synergistic effects when used in nanoparticle form in combination with cisplatin nanoparticles in vitro at a one-to-one molar ratio (IC50s = 5.95 and 34.8 for the nanoparticle combination and gemcitabine monophosphate alone, respectively). In a stroma-rich mouse xenograft model, the nanoparticle combination of gemcitabine and cisplatin inhibits tumor growth and increases apoptosis.
Brand:CaymanSKU:31726 - 1 mgAvailable on backorder
Gemcitabine monophosphate is a monophosphate form of the deoxycytidine analog gemcitabine (Item No. 9003096).{40694} It has synergistic effects when used in nanoparticle form in combination with cisplatin nanoparticles in vitro at a one-to-one molar ratio (IC50s = 5.95 and 34.8 for the nanoparticle combination and gemcitabine monophosphate alone, respectively). In a stroma-rich mouse xenograft model, the nanoparticle combination of gemcitabine and cisplatin inhibits tumor growth and increases apoptosis.
Brand:CaymanSKU:31726 - 500 µgAvailable on backorder
Gemfibrozil is a fibrate that activates peroxisome proliferator-activator α (PPARα, EC50 = 193 μM) with 100% efficacy.{23621} It also activates PPARγ (EC50 = 148 μM), but with only 79% efficacy.{23621} Presumably through its effects on PPARα, gemfibrozil lowers triglycerides and increases high density lipoprotein cholesterol levels and is used in the context of atherogenic dyslipidemia.{23620} Gemfibrozil strongly binds liver fatty acid-binding protein (Ki = 1.8 μM).{23622} Phase II metabolites of gemfibrozil inhibit certain cytochrome P450 isoforms, increasing drug-drug interaction risks.{23619}
Brand:CaymanSKU:- Gemfibrozil is a fibrate that activates peroxisome proliferator-activator α (PPARα, EC50 = 193 μM) with 100% efficacy.{23621} It also activates PPARγ (EC50 = 148 μM), but with only 79% efficacy.{23621} Presumably through its effects on PPARα, gemfibrozil lowers triglycerides and increases high density lipoprotein cholesterol levels and is used in the context of atherogenic dyslipidemia.{23620} Gemfibrozil strongly binds liver fatty acid-binding protein (Ki = 1.8 μM).{23622} Phase II metabolites of gemfibrozil inhibit certain cytochrome P450 isoforms, increasing drug-drug interaction risks.{23619}
Brand:CaymanSKU:- Gemfibrozil is a fibrate that activates peroxisome proliferator-activator α (PPARα, EC50 = 193 μM) with 100% efficacy.{23621} It also activates PPARγ (EC50 = 148 μM), but with only 79% efficacy.{23621} Presumably through its effects on PPARα, gemfibrozil lowers triglycerides and increases high density lipoprotein cholesterol levels and is used in the context of atherogenic dyslipidemia.{23620} Gemfibrozil strongly binds liver fatty acid-binding protein (Ki = 1.8 μM).{23622} Phase II metabolites of gemfibrozil inhibit certain cytochrome P450 isoforms, increasing drug-drug interaction risks.{23619}
Brand:CaymanSKU:- Gemfibrozil is a fibrate that activates peroxisome proliferator-activator α (PPARα, EC50 = 193 μM) with 100% efficacy.{23621} It also activates PPARγ (EC50 = 148 μM), but with only 79% efficacy.{23621} Presumably through its effects on PPARα, gemfibrozil lowers triglycerides and increases high density lipoprotein cholesterol levels and is used in the context of atherogenic dyslipidemia.{23620} Gemfibrozil strongly binds liver fatty acid-binding protein (Ki = 1.8 μM).{23622} Phase II metabolites of gemfibrozil inhibit certain cytochrome P450 isoforms, increasing drug-drug interaction risks.{23619}
Brand:CaymanSKU:-
Gemfibrozil 1-O-β-glucuronide is a major metabolite of gemfibrozil (Item No. 14835) that is formed when gemfibrozil undergoes glucuronidation by UDP-glucuronosyltransferase (UGT) 2B7.{37643} Gemfibrozil 1-O-β-glucuronide is an inhibitor of the cytochrome P450 (CYP) isoform CYP2C8 (IC50 = 4.1 µM). It is taken up by organic anion transporting polypeptide 1B1 (OATP1B1) in sandwich cultured human hepatocytes (SCHHs) and inhibits cellular uptake of valsartan (Item No. 14178) in MDCK cells expressing OATP1B1 (IC50 = 20.4 µM).{37644,37645}
Brand:CaymanSKU:-Available on backorder
Gemfibrozil 1-O-β-glucuronide is a major metabolite of gemfibrozil (Item No. 14835) that is formed when gemfibrozil undergoes glucuronidation by UDP-glucuronosyltransferase (UGT) 2B7.{37643} Gemfibrozil 1-O-β-glucuronide is an inhibitor of the cytochrome P450 (CYP) isoform CYP2C8 (IC50 = 4.1 µM). It is taken up by organic anion transporting polypeptide 1B1 (OATP1B1) in sandwich cultured human hepatocytes (SCHHs) and inhibits cellular uptake of valsartan (Item No. 14178) in MDCK cells expressing OATP1B1 (IC50 = 20.4 µM).{37644,37645}
Brand:CaymanSKU:-Available on backorder
Gemfibrozil-d6 is intended for use as an internal standard for the quantification of gemfibrozil (Item No. 14835) by GC- or LC-MS. Gemfibrozil is a peroxisome proliferator-activated reporter α (PPARα) and PPARγ agonist (EC50s = 193.3 and 147.8 µM, respectively, in transactivation assays).{23621} In vivo, gemfibrozil (50 mg/kg, p.o.) reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia.{54664} Gemfibrozil (100 mg/kg per day) reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif ligand 2 (CCL2) in ApoE-/- mice.{54665} Formulations containing gemfibrozil have been used in the treatment of high cholesterol.
Brand:CaymanSKU:31915 - 1 mgAvailable on backorder
Gemfibrozil-d6 is intended for use as an internal standard for the quantification of gemfibrozil (Item No. 14835) by GC- or LC-MS. Gemfibrozil is a peroxisome proliferator-activated reporter α (PPARα) and PPARγ agonist (EC50s = 193.3 and 147.8 µM, respectively, in transactivation assays).{23621} In vivo, gemfibrozil (50 mg/kg, p.o.) reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia.{54664} Gemfibrozil (100 mg/kg per day) reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif ligand 2 (CCL2) in ApoE-/- mice.{54665} Formulations containing gemfibrozil have been used in the treatment of high cholesterol.
Brand:CaymanSKU:31915 - 500 µgAvailable on backorder
Gemifloxacin is a fluoroquinolone antibiotic that is effective against C. pneumoniae and M. tuberculosis (MIC50s = 0.25 and 8 µg/ml, respectively).{29636,33222} Quinolones, including gemifloxacin, inhibit bacterial DNA gyrase and other topoisomerases.{27399,27494} Formulations containing gemifloxacin are useful against respiratory tract infections, particularly community-acquired pneumonia and tuberculosis.{29636,33220,33221}
Brand:CaymanSKU:21047 -Out of stock