SNS-032 (BMS-387032)
Catalog No.S1145
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.
4 Customer Reviews
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For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of SNS-032 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
Dr. Yong-Weon Yi from Georgetown University Medical Center. SNS-032 (BMS-387032) purchased from Selleck.
Efficacy of CDK9 inhibition in a syngeneic cancer model. Measurement of ascites fluid in the VEGF-DEF ID8 ovarian cancer mouse model is an indicator of tumor burden. In vivo treatment with the CDK9 inhibitor SNS-032 every 3 days demonstrated a decrease in tumor burden at weeks 4 and 5 (left). Addition of a-PD-1 led to a further decrease in tumor burden at week 5. Data are shown as mean + SEM (Mann-Whitney test). Survival of NSG mice was calculated using a log-rank (Mantel-Cox) test. MC180295 significantly extended survival of the mice in this model (right). In all panels, *p<0.05, **p < 0.01, ***p < 0.001. Bar graphs represent mean ± SD of at least biological triplicates.
Cell, 2018, 175(5):1244-1258. SNS-032 (BMS-387032) purchased from Selleck.
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HeLa cells were treated for 3h with PIK-75 or SNS-032 at the indicated concentrations. Cells were subsequently lysed and subjected to western blotting. One representative of two independent experiments is shown.
Cell Death Differ 2014 21(3), 491-502. SNS-032 (BMS-387032) purchased from Selleck.
Yolanda Sanchez from Geisel School of Medicine at Dartmouth. SNS-032 (BMS-387032) purchased from Selleck.
Purity & Quality Control
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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. | ||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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] |
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Solubility (25°C)
| In vitro | DMSO | 76 mg/mL (199.72 mM) |
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| 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 |
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| 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 |
Tech Support
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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