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Tankyrase-IN-2
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Tankyrase-IN-2图片
CAS NO:1588870-36-3
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Tankyrase-IN-2 (compound 5k) 是一种有效选择性的 tankyrase 抑制剂 (对 TNKS1, TNKS2, PARP1 的 IC50 值分别为 10 nM, 7 nM, 710 nM)，具有良好的理化特性和药动学特性，可调节结直肠癌异种移植模型中 Wnt 通路的活性。
Cas No.1588870-36-3
Canonical SMILESO=C1NC(C2=CC=C(C(C)(O)C)C=C2)=NC3=C1C=C(F)C=C3F
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
储存条件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
产品描述

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.