1818427-07-4
1818427-07-4 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
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CDK8/CycC 0.46 nM (IC 50 ) |
CDK19/CycC 0.99 nM (IC 50 ) |
CDK9 270 nM (IC 50 ) |
CDK8/19-IN-1 (52h) is a potent CDK8/19 dual inhibitor, with IC 50 s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively. CDK8/19-IN-1 also weakly inhibits CDK2, with 62% inhibition at 1 μM. CDK8/19-IN-1 (1 μM) shows >50% inhibition against GSK3β, PLK1, ASK1, CK1δ, PKA, ROCK1, PKCθ, CDC7. CDK8/19-IN-1 shows K d s of 25, 46, 81, 86, 97, 160 and >3000 nM for CDK19, CDK8, DYRK1B, HASPIN, YSK4, HIPK1 and EPHA3, respectively. CDK8/19-IN-1 displays potent antitumor activity, with GI 50 of 0.43-2.5 nM for colon, multiple myeloma, acute myelogenous leukemia (AML), lung cancer cells.
CDK8/19-IN-1 (52h; 1.25 mg/kg twice daily or 2.5 mg/kg once daily, p.o.) significantly suppresses tumor growth in mice bearing RPMI8226 human hematopoietic and lymphoid cells.