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].
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