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BS-181 HCl

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Chemical Structure| 1397219-81-6 同义名 : BS-181 (hydrochloride);BS-181 hydrochloride
CAS号 : 1397219-81-6
货号 : A750865
分子式 : C22H33ClN6
纯度 : 99%+
分子量 : 416.991
MDL号 : MFCD18384975
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(119.91 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(239.81 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • CDK7

    CDK7, IC50:21 nM
描述 Cyclin-dependent kinases (CDKs) are a large group of serine/threonine protein kinases that have central roles in the cell cycle signaling pathway[3]. CDK7, a member of the CDK family, can regulate transcription as part of the TFIIH basal transcription factor. BS-181 HCl inhibits cancer cell growth by inhibiting phosphorylation of CDK7 substrates, Ser5 in the RNA polymeraseII CTD. In vitro , the luciferase assay results showed that BS-181 inhibited CDK7 activity with an IC50 of 21 nM[4]. The IC50s of BS-181 HCl in MKN28, SGC-7901, AGS and BGC823 cell lines were 17-22 μM, and the IC50 in RGM-1 cell line was 6.5μM[5]. In vivo assay, tumor growth was significantly inhibited by BS-181 HCl in a dose-dependent manner. After intraperitoneal injection of BS-181 HCl to mice at the dose of 5mg / kg or 10mg / kg twice a day, the growth of tumor decreased by 25% and 50% respectively over a period of 14 days [4].
作用机制 BS-181 HCl is a highly selective CDK7 inhibitor by inhibiting phosphorylation of CDK7 substrates.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

11.99mL

2.40mL

1.20mL

23.98mL

4.80mL

2.40mL
参考文献

[1]Wang BY, Liu QY, et al. Selective CDK7 inhibition with BS-181 suppresses cell proliferation and induces cell cycle arrest and apoptosis in gastric cancer. Drug Des Devel Ther. 2016 Mar 16;10:1181-9.

[2]Ali S, Heathcote DA, et al. The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 2009 Aug 1;69(15):6208-15.

[3]Leitch AE, Haslett C, et al. Cyclin-dependent kinase inhibitor drugs as potential novel anti-inflammatory and pro-resolution agents. Br J Pharmacol. 2009; 158:1004–16.

[4]Ali S, Heathcote DA, et al. The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 2009;69(15):6208-6215

[5]Wang BY, Liu QY, et al. Selective CDK7 inhibition with BS-181 suppresses cell proliferation and induces cell cycle arrest and apoptosis in gastric cancer. Drug Des Devel Ther. 2016; 10:1181-1189