SEL120-34A HCl 是一种可口服的，选择性的，ATP-竞争性的CDK8抑制剂，具有抗肿瘤活性，对 CDK8/CycC 和 CDK19/CycC 的IC50值分别为 4.4 nM 和 10.4 nM。

SEL120-34A HCl is a selective, orally available and ATP-competitive inhibitor of CDK8(CDK8/CycC and CDK19/CycC with IC50s of 4.4 nM and 10.4 nM , respectively), with antitumor activity.

SEL120-34A HCl is a selective, ATP-competitive inhibitor of CDK8(IC50 of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively). SEL120-34A HCl is active against a panel of AML cell lines (GI50<1 μM), such as SKNO-1, KG-1, HEL-60, MOLM-16, MV-4-11, OciAML-2, MOLM-6 and OciAML-3 cells, consistent with the effective inhibition range of STAT1 S727 and STAT5 S726.

The growth of tumor in mice bearing MV4-11 cancer cells inhibited by SEL120-34A (30, 60 mg/kg, p.o.), and also arrests the growth of KG-1-derived tumors at 30 mg/kg via oral administration.

1609452-30-3

C15H18Br2N4.xHCl

DMSO:62.5 mg/mL,Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years