SEL120-34A是CDK8的选择性和ATP竞争性抑制剂，对CDK8/CycC、CDK19/CycC和CDK9/cycT的IC50s为4.4 nM、10.4 nM和1070 nM。SEL120-34A具有抗肿瘤活性。
产品描述
SEL120-34A is a selective and ATP-competitive inhibitor of CDK8 with IC50s of 4.4 nM, 10.4 nM and 1070 nM for CDK8/CycC, CDK19/CycC and CDK9/cycT. SEL120-34A possesses antitumor activity.
体外活性
SEL120-34A shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7. SEL120-34A weakly suppresses CDK9 with an IC50 of 1070 nM. SEL120-34A is active against a panel of AML cell lines including KG-1, SKNO-1, HEL-60, MOLM-16, OciAML-2, MV-4-11, MOLM-6 and OciAML-3 cells with GI50<1 μM[1].
体内活性
SEL120-34A (30 mg/kg and 60 mg/kg; p.o.) inhibits the growth of tumors in mice bearing MV4-11 cancer cells. SEL120-34A (30 mg/kg; p.o.) arrests the growth of KG-1-derived tumors[1].
Cas No.
1609522-33-9
分子式
C15H18Br2N4
分子量
414.14
储存和溶解度
DMSO:soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
