產品屬性：
產品名稱 | CAY10682 |
規格 | 1mg、5mg、10mg |
貨號 | EY-01Y16531 |
Cas No.: 1542066-74-9
別名: N/A
化學名: N/A
分子式: C30H25BrFN5O
分子量: 570.5
溶解度: DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml,Ethanol: 2 mg/ml
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway. It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKK? (IC50s = 80.5, 78.2, and 57.1 μM, respectively). CAY10682 blocks the growth of cancer cells in vitro (IC50s = 2-6 μM) and inhibits the growth of A549 cell xenografts in mice without significantly reducing body weight.
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