Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BS-181 是一种高度选择性的 CDK7 抑制剂,IC50为21 nM。它抑制CDK2、CDK5 和 CDK9 的IC50值分别为 880 nM、3000 nM 和 4200 nM 。它诱导细胞凋亡,有癌症研究相关的研究潜力。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 BS-181 hydrochloride 的水溶性和稳定性通常比游离态更好。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 待询 | ||
5 mg | ¥ 925 | 待询 | ||
10 mg | ¥ 1,510 | 待询 | ||
25 mg | ¥ 2,880 | 待询 | ||
50 mg | ¥ 5,150 | 待询 | ||
100 mg | ¥ 7,770 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 972 | 待询 |
BS-181 的其他形式现货产品:
产品描述 | BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); >40-fold selective for CDK7 than CDK1/2/4/5/6/9. |
靶点活性 | CDK7:21 nM |
体外活性 | BS-181 promotes cell cycle arrest and inhibits cancer cell growth, and growth is inhibited for all cell lines tested, with IC50 values ranging from 11.5 to 37 μM. BS-181 inhibits RB phosphorylation at Ser795 and Ser821 with an apparent IC50 of 15 μM, similar to the IC50 obtained for P-Ser2 inhibition. BS-181 treatment of MCF-7 cells leads to G1 arrest at and apoptosis[1]. BS-181 inhibits GC cell and normal gastric epithelial RGM-1 cell line growth with inhibitory concentration (IC50) ranging from 17 to 22 μM and 6.5 μM, respectively. BS-181 significantly inhibits cell migration and invasion ability in a dose-dependent manner[2]. |
体内活性 | BS-181 (5 mg/kg, 10 mg/kg, i.p.) inhibits the growth of MCF-7 tumors in nude mice. Intravenous (i.v) and i.p administration of 10 mg/kg BS-181 shows rapid clearance[1]. BS-181 (10 mg/kg/d or 20 mg/kg/d, i.p.) significantly inhibits the growth of tumor in a dose-dependent manner compared to the control group[2]. |
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 | Cell viability is detected using Cell Counting Kit (CCK-8 kit) according to supplier's introductions. Briefly, BGC823 cells are seeded at 104?cells per well for 48 hours with or without BS-181. Then, the absorbance is detected at 450 nm (reference at 650 nm) in each well. |
别名 | BS 181 |
分子量 | 380.53 |
分子式 | C22H32N6 |
CAS No. | 1092443-52-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 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 |
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 1092443-52-1 Apoptosis Cell Cycle/Checkpoint CDK Inhibitor Cyclin dependent kinase inhibit BS 181 BS181 inhibitor