SEL120-34A is a potent, selective, orally available, ATP-competitiveCDK8inhibitor, withIC₅₀s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

SEL120-34A is a selective, ATP-competitive CDK8 inhibitor, with IC₅₀of 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 stat5 s726^[1].

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].

414.14

C₁₅H₁₈Br₂N₄

1609522-33-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.