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SNS-032

Cat. No. M2065
SNS-032 Structure
Synonym:

BMS-387032

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 70  USD70 In stock
50mg USD 150  USD150 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Walsby E, et al. Leukemia. The cyclin-dependent kinase inhibitor SNS-032 has single agent activity in AML cells and is highly synergistic with cytarabine.

[2] Chen R, et al. Cancer Res. Responses in mantle cell lymphoma cells to SNS-032 depend on the biological context of each cell line.

[3] Chen R, et al. Blood. Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia.

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  Catalog
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Keywords: SNS-032, BMS-387032 supplier, CDK, inhibitors, activators


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