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.
Molecular Weight | 380.53 |
Formula | C17H24N4O2S2 |
CAS Number | 345627-80-7 |
Solubility (25°C) | DMSO 68 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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