Senexin B

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Chemical Structure| 1449228-40-3 同义名 : SNX2-1-165; BCD-115
CAS号 : 1449228-40-3
货号 : A1145598
分子式 : C27H26N6O
纯度 : 99%+
分子量 : 450.54
MDL号 : MFCD31544331
存储条件:

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Senexin B is a highly effective, selective and oral Cdk8 / cdk19 inhibitor with IC50 values ranging from 24 to 50 nm. In 8-week-old cb-17 SCID mice, 40 mg / kg senexin B or control reagent was injected intraperitoneally for 5 days, and then subcutaneously for 1 day × 106 human A549 lung cancer cell line, senexin B significantly slowed down tumor growth. In female nude mice with MDA-MB-468 three negative breast cancer (TNBC) cells injected with fat pad in situ, 25 mg/kg Senexin B (i.p.) was pretreated for 5 days a day, and the tumor growth was inhibited effectively and continuously. Senexin B is a highly effective, selective and oral Cdk8 / cdk19 inhibitor. Senexin B showed selectivity for Cdk8 and cdk19, with Kd values of 140 nm and 80 nm, respectively. 1 mm of senexin B was completely dissolved in 20% propylene glycol with a solubility of 50 mm in water. In vitro and in vivo experiments, senexin B in the low nanomolar range inhibited the activity of Cdk8 / 19 in a competitive manner of ATP[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.10mL

2.22mL

1.11mL

22.20mL

4.44mL

2.22mL

参考文献

[1]Chen M, Li J, Liang J, Thompson ZS, Kathrein K, Broude EV, Roninson IB. Systemic Toxicity Reported for CDK8/19 Inhibitors CCT251921 and MSC2530818 Is Not Due to Target Inhibition. Cells. 2019 Nov 9;8(11):1413