化合物 T22633 T22633

Product Introduction
Bioactivity


英文名: CCT251545 analogue, Compound 51

描述: CCT251545 analog is a potent and selective CDK8/19 inhibitor (IC50: 5.1 nM and 5.6 nM, respectively). Mediator complex-associated kinases CDK8 and CDK19 are involved in the regulation of multiple transcription pathways. CDK8 plays as an oncogene in gastric and colorectal cancers through the activation of WNT signaling.

体外活性: In SW620 human colorectal carcinoma cells harbouring activating APC-mutation, Compound 51 inhibited phospho-STAT1SER727 ( IC50 :17.9 nM). It is a biomarker of CDK8 inhibition [1].

体内活性: In vivo mouse and rat PK experiments, The compound demonstrated medium in vivo clearance and Vd but low bioavailability in mice. In an SW620 colorectal carcinoma human tumor xenograft model, Compound 51 (5 mg/kg p.o. dose) inhibited phospho-STAT1SER727 in a time-dependent way. Compound 51 is an advanced chemical tool to further explore the efficacy, safety, and tolerability of dual CDK8/19 ligands [1].

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

溶解度: DMSO : > 20.7 mg/mL


关键字: CCT251545 analogue, Compound 51 | CCT-251545 analogue, Compound 51

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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