CDK8/19-IN-1,1818427-07-4

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CDK8/19-IN-1

CAS No. : 1818427-07-4

MCE 国际站：CDK8/19-IN-1

产品活性：CDK8/19-IN-1 是一种有效的，选择性的，可口服的 CDK8/19 双重抑制剂，对 CDK8，CDK19 和 CDK9 的 IC₅₀ 值分别为 0.46 nM，0.99 nM 和 270 nM。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

In Vitro: CDK8/19-IN-1 (52h) is a potent CDK8/19 dual inhibitor, with IC₅₀s 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_ds 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 GI₅₀ of 0.43-2.5 nM for colon, multiple myeloma, acute myelogenous leukemia (AML), lung cancer cells.

In Vivo: 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.

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