Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 198 | 现货 | ||
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 578 | 现货 | ||
25 mg | ¥ 919 | 现货 | ||
50 mg | ¥ 1,230 | 现货 | ||
100 mg | ¥ 1,960 | 现货 | ||
200 mg | ¥ 3,730 | 现货 | ||
500 mg | ¥ 5,960 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | SNS-032 (BMS-387032) is a selective inhibitor of CDK2 (IC50: 48 nM ) and is 10- and 20-fold selective over CDK1/CDK4. It is also sensitive to CDK7/9 (IC50: 62 nM/4 nM), and no effect on CDK6. |
靶点活性 | CDK7:62 nM, CDK9:4 nM, CDK2:48 nM |
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 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] |
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) |
别名 | SNS032, BMS-387032 |
分子量 | 380.53 |
分子式 | C17H24N4O2S2 |
CAS No. | 345627-80-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 19 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6279 mL | 13.1396 mL | 26.2791 mL | 65.6978 mL |
5 mM | 0.5256 mL | 2.6279 mL | 5.2558 mL | 13.1396 mL | |
10 mM | 0.2628 mL | 1.314 mL | 2.6279 mL | 6.5698 mL | |
20 mM | 0.1314 mL | 0.657 mL | 1.314 mL | 3.2849 mL | |
50 mM | 0.0526 mL | 0.2628 mL | 0.5256 mL | 1.314 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SNS-032 345627-80-7 Apoptosis Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling Stem Cells GSK-3 CDK Cyclin dependent kinase inhibit SNS 032 Inhibitor SNS032 BMS387032 BMS 387032 BMS-387032 inhibitor