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    SNS-032 (BMS-387032)
    SNS-032 (BMS-387032)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1533
    CAS #: 345627-80-7Purity ≥98%

    Description: SNS-032 (also known as BMS-387032; SNS 032; BMS387032; SNS032), a 2-aminothiazole based small-molecule, is a potent and selective inhibitor of CDK2 (cyclin dependent kinase 2) with potential antitumor activity. It inhibits CDK2 with an IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. SNS-032 selectively binds to CDKs 2, 7, and 9, preventing their phosphorylation and activation; inhibition of CDK activity may result in cell cycle arrest, the induction of apoptosis and decreased tumor cell proliferation in susceptible tumor cell populations. This agent has been shown to sensitize radioresistant tumor cells to ionizing radiation.           

    References: Blood. 2009 May 7;113(19):4637-45; Neoplasia. 2007 May;9(5):370-81.

    Related CAS#: 345627-90-9 (HCl); 2139287-33-3 (THAL-SNS-032, a selective CDK9 degrader)

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    Molecular Weight (MW)380.53
    FormulaC17H24N4O2S2
    CAS No.345627-80-7 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 76 mg/mL (199.7 mM)
    Water: <1 mg/mL 
    Ethanol:<1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL 
    Synonyms

    BMS-387032; SNS 032; BMS387032; SNS032; BMS 387032; SNS-032

    Chemical Name: N-(5-(((5-(1,1-dimethylethyl)-2-oxazolyl)methyl)thio)-2-thiazolyl)-4-piperidinecarboxamide

    SMILES Code: O=C(C1CCNCC1)NC2=NC=C(SCC3=NC=C(C(C)(C)C)O3)S2


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    In Vitro

    In vitro activity: SNS-032 has low sensitivity to CDK1 and CDK4 with IC50 of 480 nM and 925 nM, respectively. SNS-032 effectively kills chronic lymphocytic leukemia cells in vitro regardless of prognostic indicators and treatment history. Compared with flavopiridol and roscovitine, SNS-032 is more potent, both in inhibition of RNA synthesis and at induction of apoptosis. SNS-032 activity is readily reversible; removal of SNS-032 reactivates RNA polymerase II, which led to resynthesis of Mcl-1 and cell survival. SNS-032 inhibits three dimensional capillary network formations of endothelial cells. SNS-032 completely prevents U87MG cell–mediated capillary formation of HUVECs. In addition, SNS-032 significantly prevents the production of VEGF in both cell lines, SNS-032 prevents in vitro angiogenesis, and this action is attributable to blocking of VEGF. Preclinical studies have shown that SNS-032 induces cell cycle arrest and apoptosis across multiple cell lines. SNS-032 blocks the cell cycle via inhibition of CDKs 2 and 7, and transcription via inhibition of CDKs 7 and 9. SNS-032 activity is unaffected by human serum. SNS-032 induces a dose-dependent increase in annexin V staining and caspase-3 activation. At the molecular level, SNS-032 induces a marked dephosphorylation of serine 2 and 5 of RNA polymerase (RNA Pol) II and inhibits the expression of CDK2 and CDK9 and dephosphorylated CDK7.


    Kinase Assay: SNS-032 is a selective inhibitor of CDK2, CDK7, and CDK9 with IC50s of 38 nM, 62 nM and 4 nM, respectively.


    Cell Assay: CLL cells treated with SNS-032 for 6 or 24 hrs showed a decrease in the phosphorylation of Ser2 and Ser5 of the CTD of RNA Pol II, which appeared to be both time- and concentration- dependent, and remarkably consistent among samples. For the phosphorylation of Ser2, the inhibition of SNS-032 was greater than that for the phosphorylation of Ser5, this was consistent with the fact that IC50 for the inhibition of CDK9 was lower compared with that for the inhibition of CDK7 (4 nM vs 62 nM). After 6 hrs of SNS-032 exposure, protein levels of CDK7 and CDK9 were stable, but declined at 24 hrs.

    In VivoSNS-032 prevents tumor cell-induced VEGF secretion in a tumor coculture model. SNS-032, a new CDK inhibitor, is more selective and less cytotoxic and has been shown to prolong stable disease in solid tumors.
    Animal modelMDA-MB-435 xenograft mouse model
    Formulation & Dosage15 mg/kg; i.p.; every 3 days for approximately one month
    ReferencesBlood. 2009 May 7;113(19):4637-45; Neoplasia. 2007 May;9(5):370-81.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    SNS-032 (BMS-387032)

     

    SNS-032 (BMS-387032)



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