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CDK8/19-IN-2 (compound 12) is an orally active and potent cyclin-dependent kinase 8/19 (CDK8 and CDK19) inhibitor, with IC50 values of 2.08 and 2.49 nM, respectively. CDK8/19-IN-2 can be used for acute myeloid leukemia (AML), breast cancer, and lymphoma research[1]. | [in vivo]
CDK8/19-IN-2 (compound 12) (3-10 mg/kg, orally by gavage, once per day) inhibits tumor growth[1]. | Animal Model: | Female BALB/c nude mice (6-8 weeks, human AML cell line MV4-11 were inoculated subcutaneously at the right flanks of animals)[1] | | Dosage: | 3 mg/kg, 10 mg/kg | | Administration: | orally by gavage, once per day | | Result: | Resulted in a dose-dependent inhibition of tumor growth, reaching end point tumor growth inhibition (TGI) of 29%, and 76% at 3 and 10 mg/kg, respectively, without affecting body weight. |
| [IC 50]
CDK8/CycC: 2.08 nM (IC50); CDK19/CycC: 2.49 nM (IC50) | [References]
[1] Xu J, et al. Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of Cancer. J Med Chem. 2024 May 23;67(10):8161-8171. DOI:10.1021/acs.jmedchem.4c00248 |
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