SNS-032 (BMS-387032)

Catalog No.S1145

SNS-032 (BMS-387032) Chemical Structure

Molecular Weight(MW): 380.53

SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. Phase 1.

Size Price Stock Quantity  
In DMSO USD 170 In stock
USD 110 In stock
USD 170 In stock
USD 570 In stock
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Cited by 20 Publications

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Biological Activity

Description SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. Phase 1.
Targets
CDK9/CyclinT [3]
(Cell-free assay)		 CDK2/CyclinA [3]
(Cell-free assay)		 CDK2/CyclinE [1]
(Cell-free assay)		 CDK7/CyclinH [3]
(Cell-free assay)		 GSK-3α [3]
(Cell-free assay)
4 nM 38 nM 48 nM 62 nM 230 nM
In vitro

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. [1] 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. [2] 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. [3]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. [4]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A2780 cell line MofBVJJwdGmoZYLheIlwdiCjc4PhfS=> NInJPJY4OiCq MkHpRY51cXC{b3zp[oVz[XSrdnWg[YZn\WO2IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdCCuaX7lJJdieyCmZYTldo1qdmWmIHnuJIEhf2ixbHWgZ4VtdCB5MjDodkBkgXSxdH;4bYNqfHliYYPzZZktKEmFNUC9PVUhdk1? NXPuXoVbOTVyMke4OlM>
human HCT116 cells MljtSpVv[3Srb36gZZN{[Xl? NVHUZ4dnUW6qaXLpeIlwdiCxZjDDSGs6KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{BxcG:|cHjvdk1{\XJ{IHzleoVtKG:oIGLORUBxd2y7bXXyZZNmKDJiYX\0[ZIhOTZiaILzJIJ6KGirZ3igZ49vfGWwdDDj[YxtfWyjcjDhd5NigSxiSVO1NF01PThibl2= NYm4TXI6OTh6NEK0NFk>
human HCT116 cells M1XsUGZ2dmO2aX;uJIF{e2G7 MXOxOkBp NYHOT5JJUW6qaXLpeIlwdiCxZjDDSGs6NW2nZHnheIVlKFKQQTDwc4whOiCyaH;zdIhwenmuYYTpc44h[XRic3XyNkBqdiCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhOTZiaILzJIJ6KEiFUzDhd5NigSxiSVO1NF0xNjV3IN88US=> MkjwNVg6OjZ4OUm=

... Click to View More Cell Line Experimental Data
In vivo SNS-032 prevents tumor cell-induced VEGF secretion in a tumor coculture model. [2] SNS-032, a new CDK inhibitor, is more selective and less cytotoxic and has been shown to prolong stable disease in solid tumors. [4]

Protocol

Cell Research:[2]
+ Expand
  • Cell lines: HUVECs and U87MG cells
  • Concentrations: 0–0.5 mM
  • Incubation Time: 24, 48, or 72 hours
  • Method: Cell Titer-Glo (CTG) luminescent assay is performed to measure the growth curves of both HUVECs and U87MG cells. U87MG cells and HUVECs (2×103 cells/well) are seeded in a 96-well microplate in a final volume of 100 ml. After 24 hours, cells are treated with various doses of SNS-032 (0–0.5 mM) for 24, 48, or 72 hours. After completion of the treatment, 100 ml of CTG solution is added to each well and incubated for 20 minutes at room temperature in the dark. Lysate (50 ml) is transferred to a 96-well white plate, and luminescence is measured by POLARstar OPTIMA. Percent cell growth is calculated by considering 100% growth at the time of SNS-032 addition.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (199.72 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing. 		30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 380.53
Formula

C17H24N4O2S2
CAS No. 345627-80-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00446342 Completed B-lymphoid Malignancies|Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma|Multiple Myeloma Sunesis Pharmaceuticals February 2007 Phase 1
NCT00446342 Completed B-lymphoid Malignancies|Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma|Multiple Myeloma Sunesis Pharmaceuticals February 2007 Phase 1
NCT00292864 Completed Tumors Sunesis Pharmaceuticals January 2006 Phase 1
NCT00292864 Completed Tumors Sunesis Pharmaceuticals January 2006 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID