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CAS No.: 1397219-81-6

BS-181 HCl Catalog No. CSN17151

Synonyms: BS-181 (hydrochloride);BS-181 HCl

BS-181 is a selective CDK7 inhibitor with IC50 of 21 nM.

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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.
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3981 mL
- 11.9907 mL
- 23.9814 mL
- 5 mM
- 0.4796 mL
- 2.3981 mL
- 4.7963 mL
- 10 mM
- 0.2398 mL
- 1.1991 mL
- 2.3981 mL

技术信息

CAS号

1397219-81-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H33ClN6

运输

蓝冰

分子量

416.99

别名

BS-181 (hydrochloride);BS-181 HCl

溶解度

DMSO	83.0 mg/mL (199.0 mM)
Ethanol	22.0 mg/mL (52.8 mM) warming

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