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CCT-251921

    
98%

CCT-251921

源葉(MedMol)
S83682 一鍵復制產品信息
1607837-31-9
C21H23ClN6O
410.8999
貨號 規格 價格 上海 北京 武漢 南京 購買數量
S83682-1mg 98% ¥900.00 貨期:2-3天 - - -
S83682-5mg 98% ¥2400.00 貨期:2-3天 - - -
S83682-10mg 98% ¥3500.00 貨期:2-3天 - - -
S83682-25mg 98% ¥7000.00 貨期:2-3天 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

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

產品描述: CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.
靶點: CDK8:2.3 nM (IC50);CDK19:2.6 nM (IC50);CDK
體外研究: 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
體內研究: 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
參考文獻: 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
保存條件: -20℃
配置溶液濃度參考:
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: 部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。

參考文獻

質檢證書(COA)

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批號:JS298415 貨號:S20001-25g
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摩爾濃度計算器

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