1588870-36-3

1588870-36-3 structure

Name: Tankyrase-IN-2
Chemical Name: Tankyrase-IN-2
CAS Number: 1588870-36-3
Molecular Formula: C₁₇H₁₄F₂N₂O₂
Molecular Weight: 316.30
Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
Create Date: 2019-09-07 15:17:19
Modify Date: 2024-01-15 12:05:50
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].

Name	Tankyrase-IN-2

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Epigenetics >> PARP Signaling Pathways >> Cell Cycle/DNA Damage >> PARP
Target	IC50: 10 nM (TNKS1), 7 nM (TNKS2), 710 nM (PARP1)[1]
In Vitro	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].
References	[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.

Molecular Formula	C₁₇H₁₄F₂N₂O₂
Molecular Weight	316.30