tcsc0040310 SEL120-34A

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

IC50 & Target: IC50: 4.4 nM (CDK8/CycC), 10.4 nM (CDK19/CycC)^[1]

In Vitro: SEL120-34A is a selective, ATP-competitive CDK8 inhibitor, with IC₅₀ of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively. SEL120-34A shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC₅₀, 1070 nM). SEL120-34A 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^[1].

In Vivo: SEL120-34A (30, 60 mg/kg, p.o.) inhibits the growth of tumor in mice bearing MV4-11 cancer cells, and also arrests the growth of KG-1-derived tumors at 30 mg/kg via oral administration^[1].