Dacarbazine-d6 is intended for use as an internal standard for the quantification of dacarbazine (Item No. 21877) by GC- or LC-MS. Dacarbazine is a DNA alkylating prodrug that is activated by P450 enzymes in liver microsomes.{21297} Following activation, it is converted, through a series of reactions, into a methyldiazonium cation that alkylates DNA at all phases of the cell cycle and induces apoptosis. In vitro, dacarbazine inhibits the growth of B16/F1, A-875, and SK-MEL-5 melanoma and non-cancerous WI-38 lung fibroblast and L-02 hepatocyte cell lines (IC50s = 260, 287, 380, 526, and 367 μM, respectively).{41584} Dacarbazine toxicity to 518A2 and SK-MEL-28 melanoma cell lines increases in a time-dependent manner with IC50 values of 121 and >400 μM, respectively, following a 1 hour incubation and 2.5 and 50 μM, respectively, following a 96 hour incubation.{41585} In vivo, dacarbazine (70 mg/kg, once every 2 days) decreases tumor volume by 59.1% in a B16/F1 murine melanoma model in mice.{41584} Formulations containing dacarbazine have been used in the treatment of metastatic melanoma and for Hodgkin’s lymphoma in combination with other antineoplastic agents.
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An internal standard for the quantification of dacarbazine by GC- or LC-MS
Formal name: 5-(3,3-dimethyl-1-triazen-1-yl)-1H-imidazole-4-d6-carboxamide
Synonyms:
Molecular weight: 188.2
CAS: 1185241-28-4
Purity: ≥99% deuterated forms (d1-d6)
Formulation: A solid
The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
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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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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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