Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BS-181 hydrochloride (BS-181 HCl) 是一种高度选择性的CDK7抑制剂,IC50值为 21 nM。它对 CDK7 的选择性是对 CDK1、2、4、5、6 和 9 的 40 倍以上。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 283 | 现货 | ||
2 mg | ¥ 395 | 现货 | ||
5 mg | ¥ 652 | 现货 | ||
10 mg | ¥ 898 | 现货 | ||
25 mg | ¥ 1,880 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,370 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
产品描述 | BS-181 hydrochloride (BS-181 HCl) is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9. |
靶点活性 | CDK7:21 nM |
体外活性 | BS-181 is a small molecule inhibitor of CDK7 in a cell-free environment, which displays more potential activity than roscovitine with IC 50 of 510 nM. Among the CDKs and other 69 kinases from many different classes, BS-181 shows high inhibitory selectivity for CDK7, inhibits CDK2 at concentrations lower than 1 μM which being inhibited 35-fold less potently (IC50 with 880 nM) than CDK7, shows slight inhibition for CDK1, CDK4, CDK5, CDK6 and CDK9 with IC50 values higher than 3.0 μM, and only shows inhibition for several kinases from other classes at high concentrations (>10 μM). BS-181 promotes cell cycle arrest and inhibits the cancer cell growth of a range of tumor types, including breast, lung, prostate and colorectal cancer with IC50 in the range of 11.5-37 μM. In MCF-7 cells, BS-181 inhibits the phosphorylation of the CDK7 substrate RNA polymerase II COOH-terminal domain (CTD), and promotes cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines. [1] |
体内活性 | BS-181 is stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. BS-181 inhibits the growth of MCF-7 xenografts in the nude mice model in a dose-dependent manner, with 25% and 50% reduction in tumor growth after 2 weeks of treatment at 10 mg/kg/day and 20 mg/kg/day, respectively without apparent toxicity. [1] |
激酶实验 | In vitro kinase inhibition.: Inhibition of CDK7 activity is measured by incubation of increasing amounts of BS-181 with purified recombinant CDK7/CycH/MAT1 complex, followed by measurement of free ATP remaining in the reaction using a luciferase assay, luciferase activity therefore providing a measure of inhibition of CDK7 activity for the determination of IC50. |
细胞实验 | MCF-7 cells are exposed to BS-181 for 24 hours. For the determination of cell cycle and apoptosis, cells are stained with propidium iodide or labeled with Annexin V-FITC, then labeled cells are acquired within 1 hour, by using the RXP cytomics software on a Beckman Coulter Elite ESP, and the data are analyzed using Flow Jo v7.2.5. For the assessment of CDKs, cells are lysed and analyzed by western blotting.(Only for Reference) |
别名 | BS-181 HCl |
分子量 | 416.99 |
分子式 | C22H32N6·HCl |
CAS No. | 1397219-81-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 22 mg/mL (52.75 mM), Heating is recommended.
H2O: 3 mg/mL (7.19 mM)
DMSO: 83 mg/mL (199.04 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / H2O / DMSO | 1 mM | 2.3981 mL | 11.9907 mL | 23.9814 mL | 59.9535 mL |
5 mM | 0.4796 mL | 2.3981 mL | 4.7963 mL | 11.9907 mL | |
Ethanol / DMSO | 10 mM | 0.2398 mL | 1.1991 mL | 2.3981 mL | 5.9953 mL |
20 mM | 0.1199 mL | 0.5995 mL | 1.1991 mL | 2.9977 mL | |
50 mM | 0.048 mL | 0.2398 mL | 0.4796 mL | 1.1991 mL | |
DMSO | 100 mM | 0.024 mL | 0.1199 mL | 0.2398 mL | 0.5995 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。
BS-181 hydrochloride 1397219-81-6 Cell Cycle/Checkpoint CDK BS181 Hydrochloride BS-181 BS181 Inhibitor inhibit BS-181 HCl BS 181 hydrochloride Cyclin dependent kinase BS 181 Hydrochloride BS-181 Hydrochloride BS 181 BS181 hydrochloride inhibitor