產(chǎn)品屬性：
產(chǎn)品名稱 | Tankyrase-IN-2 |
規(guī)格 | 100mg、250mg、500mg |
貨號 | EY-01Y12952 |
Cas No.: 1588870-36-3
別名: N/A
化學(xué)名: N/A
分子式: C17H14F2N2O2
分子量: 316.3
溶解度: DMF: 10mg/mL,DMSO: 10mg/mL,Ethanol: 10mg/mL,Ethanol:PBS (pH 7.2) (1:30): 0.025mg/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(chǎn)品描述：
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model[1].IC50: 10 nM (TNKS1), 7 nM (TNKS2), 710 nM (PARP1)[1]Tankyrase-IN-2 (1-10000 nM; 24 hours) leads to a dose-dependent increase of tankyrase protein abundance with an EC50 of 320 nM in DLD1 cells. This is in the same potency range as the value for axin2 increase (EC50=319 nM)[1].[1]. Buchstaller HP, et al. Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective TankyraseInhibitor Modulating Wnt Pathway Activity. J Med Chem. 2019 Aug 5.
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