货号	规格	价格	上海	北京	珠海	重庆	武汉
S83682-1mg	≥98%	￥790.00 S83682-1mg ￥790.00 3-5天	0 货期：3-5天	-	-	-	-
S83682-5mg	≥98%	￥1560.00 S83682-5mg ￥1560.00 3-5天	0 货期：3-5天	-	-	-	-
S83682-10mg	≥98%	￥2350.00 S83682-10mg ￥2350.00 3-5天	0 货期：3-5天	-	-	-	-
S83682-25mg	≥98%	￥4230.00 S83682-25mg ￥4230.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.

靶点：

CDK8:2.3 nM (IC50);CDK19:2.6 nM (IC50);CDK

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

参考文献：

1. Mallinger A, et al. Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. J Med Chem. 2016 Feb 11;59(3):1078-101.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.434 ml	12.168 ml	24.337 ml
5 mM	0.487 ml	2.434 ml	4.867 ml
10 mM	0.243 ml	1.217 ml	2.434 ml
50 mM	0.049 ml	0.243 ml	0.487 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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