Tankyrase-IN-2

A TNKS1/2 inhibitor

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100mg

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货号: ajce59712
CAS: 1588870-36-3
别名:
分子式: C17H14F2N2O2
分子量: 316.3
纯度: >98%
溶解度: DMF: 10mg/mL,DMSO: 10mg/mL,Ethanol: 10mg/mL,Ethanol:PBS (pH 7.2) (1:30): 0.025mg/mL
储存: Store at -20°C
库存: 现货

Background

Tankyrase-IN-2 is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC₅₀s = 7 and 9.2 nM, respectively).¹ It is selective for TNKS1 and TNKS2 over a panel of 10 additional poly(ADP-ribose) polymerases (PARPs; IC₅₀s = 710->10,000 nM for the human enzymes). Tankyrase-IN-2 increases accumulation of Axin2 and TNKS, indicating inhibition of TNKS-mediated auto-PARsylation, in DLD-1 colorectal cancer cells with EC₅₀ values of 319 and 320 nM, respectively. It also increases tumor Axin2 and TNKS accumulation, as well as decreases tumor levels of active β-catenin, in a DLD-1 mouse xenograft model when administered at doses of 10, 30, and 90 mg/kg.

1.Buchstaller, H.-P., Anlauf, U., Dorsch, D., et al.Discovery and optimization of 2-arylquinazolin-4-ones into a potent and selective tankyrase inhibitor modulating Wnt pathway activityJ. Med. Chem.62(17)7897-7909(2019)