化合物SNS032 T6049

Product Introduction
Bioactivity


英文名: SNS-032

描述: SNS-032 (BMS-387032) 是选择性的CDK2/7/9有效抑制剂，IC50值分别为 48 nM/62 nM/4 nM。它有抗肿瘤作用。

细胞实验: Cell Titer-Glo (CTG) luminescent assay is performed to measure the growth curves of both HUVECs and U87 mg cells. U87 mg 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)

体外活性: 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 U87 mg 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. PreClinicalal 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]

体内活性: SNS-032 在肿瘤共培养模型中防止了肿瘤细胞诱导的VEGF分泌。[2] 作为一种新型CDK抑制剂，SNS-032展现出更高的选择性和较低的细胞毒性，已被证明能够在实体肿瘤中延长疾病的稳定状态。[4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 16.67 mg/mL (43.8 mM)


关键字: Cyclin dependent kinase | inhibit | SNS 032 | Inhibitor | CDK | BMS387032 | Apoptosis | BMS 387032 | SNS-032

相关产品: Protosappanin B | TMI-1 | Salinomycin sodium salt | 4-Thiothymidine | PR-619 | Busulfan | SW106065 | kauran-16,17-diol | Bcl-B inhibitor 1 | Evocarpine

相关库: Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | Glycometabolism Compound Library | Anti-Cancer Drug Library | Anti-Lung Cancer Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library

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