Ceritinib-d7 is intended for use as an internal standard for the quantification of ceritinib (Item No. 19374) by GC- or LC-MS. Ceritinib is an inhibitor of anaplastic lymphoma kinase (ALK; IC50 = 0.2 nM).{48716} It is selective for ALK over IGF-1R, InsR, STK22D, and FLT3 (IC50s = 8, 7, 23, and 60 nM, respectively) as well as a panel of 25 additional kinases (IC50s = >0.26 μM for all). Ceritinib inhibits the proliferation of Ba/F3 cells expressing the fusion protein nucleophosmin-ALK (NPM-ALK) or echinoderm microtubule-associated protein-like 4-ALK (ELM4-ALK; IC50s = 0.02 and 0.021 μM, respectively), as well as several crizotinib-resistant NPM-ALK and ELM4-ALK mutants.{31295} It reduces tumor growth in an H2228 non-small cell lung cancer (NSCLC) rat xenograft model when administered at a dose of 10 mg/kg per day and induces tumor regression at 25 mg/kg per day.{48716} Ceritinib (25 and 50 mg/kg per day) also induces tumor regression in a Karpas299 lymphoma rat xenograft model. Formulations containing ceritinib have been used in the treatment of ALK-positive metastatic NSCLC.
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An internal standard for the quantification of ceritinib by GC- or LC-MS
Formal name: 5-chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-[1-(methyl-d3)ethoxy-1,2,2,2-d4]-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine
Synonyms: LDK 378-d7
Molecular weight: 565.2
CAS: 1632484-77-5
Purity: ≥99% deuterated forms (d1-d7)
Formulation: A solid
Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
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The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.
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