SNS-032 (formerly BMS-387032) is a small-molecule cyclin-dependent kinases (CDK) inhibitor. SNS-032 arrests the cell cycle at G2/M; inhibits transcription, proliferation and colony formation, and induces apoptosis in RPMI-8226 multiple myeloma cells. SNS-032 (BMS-387032) prevents tumor cell-induced VEGF secretion and in vitro angiogenesis. SNS-032-induced a dose-dependent increase in annexin V staining and caspase-3 activation. At the molecular level, SNS-032 induced a marked dephosphorylation of serine 2 and 5 of RNA polymerase (RNA Pol) II and inhibited the expression of CDK2 and CDK9 and dephosphorylated CDK7. SNS-032 effectively killed chronic lymphocytic leukemia cells in vitro. At the dose levels tested, the oral bioavailability of SNS-032 ranged from 4-33%. SNS-032 is currently in phase I clinical trials for the treatment of B-cell malignancies and advanced solid tumors.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
The cyclin-dependent kinase inhibitor SNS-032 has single agent activity in AML cells and is highly synergistic with cytarabine.
Walsby E, et al. Leukemia. 2011 Mar;25(3):411-9. PMID: 21212792.
Responses in mantle cell lymphoma cells to SNS-032 depend on the biological context of each cell line.
Chen R, et al. Cancer Res. 2010 Aug 15;70(16):6587-97. PMID: 20663900.
Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia.
Chen R, et al. Blood. 2009 May 7;113(19):4637-45. PMID: 19234140.
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