化合物 T10739 T10739

Product Introduction
Bioactivity


英文名: CDK8/19-IN-1

描述: CDK8/19-IN-1 is a selective and oral bioavailable CDK8/19 dual inhibitor (IC50s: 0.46 nM, 0.99 nM, and 270 nM for CDK8, CDK19, and CDK9).

体外活性: CDK8/19-IN-1 (52h) 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 Kds 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 (GI50: 0.43-2.5 nM for colon, multiple myeloma, acute myelogenous leukemia (AML), lung cancer cells).

体内活性: In mice bearing RPMI8226 human hematopoietic and lymphoid cells, CDK8/19-IN-1 (1.25 mg/kg twice daily or 2.5 mg/kg once daily, p.o.) significantly suppresses tumor growth.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: CDK8/19IN1 | CDK8/19-IN-1 | CDK-8/19-IN-1 | CDK8/19 IN 1

相关产品: Ribociclib hydrochloride | THAL-SNS-032 | CDK8-IN-13 | FMF-04-159-2 | (R)-Simurosertib | CDK2-IN-20 | Pinoresinol | Olomoucine | Cdc7-IN-5 | CDK9-IN-15

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途