BMS-387032
N-[5-[(5-tert-Butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide
CAS: 345627-80-7
Molecular Formula: C17H24N4O2S2
BMS-387032 - Names and Identifiers
BMS-387032 - Physico-chemical Properties
| Molecular Formula | C17H24N4O2S2 |
| Molar Mass | 380.53 |
| Density | 1.28±0.1 g/cm3(Predicted) |
| Melting Point | 171-173 °C |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 7.33±0.70(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| Refractive Index | 1.606 |
| In vitro study | SNS-032 is a novel potent selective Cdk inhibitor that effectively inhibits Cdk2, Cdk7, and cdk9. In vitro, SNS-032 were effective in killing chronic lymphocytic leukemia cells regardless of predisposition and history of treatment. Inhibition of RNA synthesis and induction of apoptosis were SNS-032 more effective than flavopidol and Roscovitine. SNS-032 is reversible, inactivating SNS-032 reactivated RNA polymerase II, resulting in Mcl-1 resynthesis and cell survival. SNS-032 inhibits the formation of a three-dimensional capillary network of endothelial cells. SNS-032 acts on human umbilical vein endothelial cells (HUVECs) to completely inhibit U87MG cell-mediated capillary formation. In addition, SNS-032 significantly inhibited the production of VEGF, thereby inhibiting angiogenesis. Preclinical studies showed that SNS-032 induce cell cycle arrest and apoptosis across multiple cell lines. SNS-032 block the cell cycle by inhibiting CDKs 2 and 7, and block transcription by inhibiting CDKs 7 and 9. SNS-032 of the activity was not affected by human serum. SNS-032 induced increased annexin V staining and caspase-3 activation in a dose-dependent manner. At the molecular level, SNS-032 induced the dephosphorylation of RNA polymerase (RNA Pol) II at serine 2 and 5 sites. And inhibit CDK2, cdk9. And the expression of dephosphorylated cdk7. SNS-032 is a novel potent and selective Cdk inhibitor that effectively inhibits Cdk2, Cdk7 and cdk9. In vitro, SNS-032 were effective in killing chronic lymphocytic leukemia cells regardless of predisposition and history of treatment. Inhibition of RNA synthesis and induction of apoptosis were SNS-032 more effective than flavopidol and Roscovitine. SNS-032 is reversible, inactivating SNS-032 reactivated RNA polymerase II, resulting in Mcl-1 resynthesis and cell survival. SNS-032 inhibits the formation of a three-dimensional capillary network of endothelial cells. SNS-032 acts on human umbilical vein endothelial cells (HUVECs) to completely inhibit U87MG cell-mediated capillary formation. In addition, SNS-032 significantly inhibited the production of VEGF, thereby inhibiting angiogenesis. Preclinical studies showed that SNS-032 induce cell cycle arrest and apoptosis across multiple cell lines. SNS-032 block the cell cycle by inhibiting CDKs 2 and 7, and block transcription by inhibiting CDKs 7 and 9. SNS-032 of the activity was not affected by human serum. SNS-032 induced increased annexin V staining and caspase-3 activation in a dose-dependent manner. At the molecular level, SNS-032 induced the dephosphorylation of RNA polymerase (RNA Pol) II at serine 2 and 5 sites. And inhibit CDK2, cdk9. And the expression of dephosphorylated cdk7. |
| In vivo study | SNS-032 acts on the tumor co-culture model, blocking tumor cell-induced VEGF secretion. SNS-032, the effect on solid tumors has a higher selectivity, and the toxicity is weak. SNS-032 acts on the tumor co-culture model and blocks VEGF secretion induced by tumor cells. SNS-032, the effect on solid tumors has a higher selectivity, and the toxicity is weak. |
BMS-387032 - Risk and Safety
| HS Code | 29349990 |
BMS-387032 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.628 ml | 13.14 ml | 26.279 ml |
| 5 mM | 0.526 ml | 2.628 ml | 5.256 ml |
| 10 mM | 0.263 ml | 1.314 ml | 2.628 ml |
| 5 mM | 0.053 ml | 0.263 ml | 0.526 ml |
Last Update：2024-01-02 23:10:35
BMS-387032 - Reference Information
| biological activity | SNS-032 (BMS-387032) is a selective CDK2 inhibitor with IC50 of 48 nM, 10 and 20 times higher selectivity than CDK1/CDK4, respectively. Sensitive to CDK7/9, IC50 is 62 nM/4 nM, and there is little inhibitory effect on CDK6. Phase 1. SNS-032 (BMS-387032) was originally described as a selective CDK2 inhibitor. IC50 was 48 nM in cell-free test, which was 10 and 20 times more selective than CDK1/CDK4. It was also sensitive to CDK7/9 with an IC50 of 62 nM/4 nM and had little inhibitory effect on CDK6. SNS-032 (BMS-387032) can induce apoptosis. Phase 1. |
| in vitro study | SNS-032 is a new and effective selective Cdk inhibitor, effectively inhibiting Cdk2, Cdk7 and Cdk9. In vitro, SNS-032 can effectively kill chronic lymphocytic leukemia cells regardless of the condition and treatment history. Compared with Flavopiridol and Roscovitine, SNS-032 is more effective when inhibiting RNA synthesis and inducing apoptosis. The SNS-032 is reversible, inactivating SNS-032 reactivating RNA polymerase II, leading to Mcl-1 resynthesis and cell survival. SNS-032 inhibits the formation of three-dimensional capillary network of endothelial cells. SNS-032 acts on human umbilical vein endothelial cells (HUVECs) to completely inhibit capillary formation regulated by U87MG cells. In addition, SNS-032 significantly inhibited the production of VEGF, thereby inhibiting angiogenesis. Pre-clinical studies have shown that SNS-032 induce cell cycle arrest and apoptosis across multiple cell lines. SNS-032 block the cell cycle by inhibiting CDKs 2 and 7, and block transcription by inhibiting CDKs 7 and 9. The activity of SNS-032 is not affected by human serum. SNS-032 induce increased staining and caspase-3 activation of conjugin V, which is dose-dependent. At the molecular level, SNS-032 induces RNA polymerase (RNA Pol) II dephosphorylation at serine 2 and 5 sites. And inhibit CDK2,CDK9. and dephosphorylated CDK7 expression. SNS-032 is a new and effective selective Cdk inhibitor, effectively inhibiting Cdk2, Cdk7 and Cdk9. In vitro, SNS-032 can effectively kill chronic lymphocytic leukemia cells regardless of the condition and treatment history. Compared with Flavopiridol and Roscovitine, SNS-032 is more effective when inhibiting RNA synthesis and inducing apoptosis. The SNS-032 is reversible, inactivating SNS-032 reactivating RNA polymerase II, leading to Mcl-1 resynthesis and cell survival. SNS-032 inhibits the formation of three-dimensional capillary network of endothelial cells. SNS-032 acts on human umbilical vein endothelial cells (HUVECs) to completely inhibit capillary formation regulated by U87MG cells. In addition, SNS-032 significantly inhibited the production of VEGF, thereby inhibiting angiogenesis. Pre-clinical studies have shown that SNS-032 induce cell cycle arrest and apoptosis across multiple cell lines. SNS-032 block the cell cycle by inhibiting CDKs 2 and 7, and block transcription by inhibiting CDKs 7 and 9. The activity of SNS-032 is not affected by human serum. SNS-032 induce increased staining and caspase-3 activation of conjugin V, which is dose-dependent. At the molecular level, SNS-032 induces RNA polymerase (RNA Pol) II dephosphorylation at serine 2 and 5 sites. And inhibit CDK2,CDK9. and dephosphorylated CDK7 expression. |
| in vivo study | SNS-032 act on tumor co-culture model to block VEGF secretion induced by tumor cells. SNS-032, it has higher selectivity and weak toxicity when acting on solid tumors. SNS-032 acts on tumor co-culture model to block VEGF secretion induced by tumor cells. SNS-032, it has higher selectivity and weak toxicity when acting on solid tumors. |
| features | SNS-032 is a new generation of CDK inhibitors with higher selectivity and weaker toxicity. |
| target | TargetValue CDK9/CyclinT (cell-free assay) 4 nM CDK2/CyclinA (cell-free assay) 38 nM CDK2/CyclinE (cell-free assay) 48 nM CDK7/CyclinH (cell-free assay) 62 nM GSK-3α (cell-free assay) 230 nM |
| Target | Value |
| CDK9/CyclinT (Cell-free assay) | 4 nM |
| CDK2/CyclinA (Cell-free assay) | 38 nM |
| CDK2/CyclinE (Cell-free assay) | 48 nM |
| CDK7/CyclinH (Cell-free assay) | 62 nM |
| GSK-3α (Cell-free assay) | 230 nM |
Last Update：2024-04-09 15:16:35
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Tel: +86-18821248368
Email: Int06@meryer.com
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Product Name: SNS-032 Request for quotationCAS: 345627-80-7
Tel: 400-968-2212
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Mobile: 18916960931
QQ: 3623107365
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Product Name: SNS-032 (BMS-387032) Visit Supplier Webpage Request for quotationCAS: 345627-80-7
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
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Multiple SpecificationsSpot supply
Product Name: BMS-387032 Visit Supplier Webpage Request for quotationCAS: 345627-80-7
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: SNS-032 Visit Supplier Webpage Request for quotationCAS: 345627-80-7
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185
Wechat: chinaskyrun
Product Name: SNS-032 (BMS-387032) Visit Supplier Webpage Request for quotation
CAS: 345627-80-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 345627-80-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
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