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CCT251921,1607837-31-9

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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
    ConcentrationSolventMass1 mg5 mg10 mg
    1 mM2.4337 mL12.1684 mL24.3368 mL
    5 mM0.4867 mL2.4337 mL4.8674 mL
    10 mM0.2434 mL1.2168 mL2.4337 mL
    *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:

      产品货号   产品名称   规格 价格 大包装及货期
      abs814401   CCT251921   50mg  8550   立即咨询

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