CCT251921,1607837-31-9
- 品牌:absin
- 型号:abs814401
- 产地:中国
- 供应商:爱必信(上海)生物科技有限公司
- 供应商报价:¥8550
- 标签:CCT251921,1607837-31-9、CCT251921,1607837-31-9价格、CCT251921,1607837-31-9厂家、CCT-251921,CCT 251921、Absin、爱必信(上海)生物科技有限公司
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YZ剂描述: 产品名称:CCT251921 产品别名:CCT-251921,CCT 251921 英文别名:CCT-251921;CCT 251921 靶点:CDK CAS:1607837-31-9 纯度:>98% 外观:Powder 保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述:CCT251921 is a potent, selective, and orally bioavailable small-molecule modulators of the mediator complex-associated kinases CDK8 and CDK19. (IC50 data: CDK8:=2.3 nM; CDK19 = 2.6 nM). 溶解性: In Vitro: DMSO : ≥ 28 mg/mL (68.14 mM) * "≥" means soluble, but saturation unknown. Preparing Stock Solutions
*请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存方式和期限。 体外研究: CCT-251921 has acceptable aqueous solubility and demonstrates minimal activity when tested in a panel of 55 receptors, ion channels, and enzymes at 1 μM and in a panel of 279 kinases; weak inhibition of CYPs is observed. CCT-251921 demonstrates potent inhibition of reporter-based readouts measuring basal WNT pathway activity in human cancer cell lines that have constitutively activated WNT pathway signaling: LS174T (β-catenin mutant), SW480 and Colo205 (APC mutant) or PA-1 human teratocarcinoma cells that are WNT ligand dependent. 体内研究: CCT-251921 shows improved oral pharmacokinetics and pharmaceutical properties in order to facilitate further evaluation of CDK8/19 pharmacology and progression into preclinical efficacy and safety studies. In APC-mutant SW620 human colorectal carcinoma xenograft model, CCT-251921 treatment reduces mice tumor weight (54.2%) at day 15. The inhibition of STAT1SER727 phosphorylation is maintained for more than 6 h after the last dose. 产品信息订购:
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