Tankyrase-IN-2

Names

[ Name ]:
Tankyrase-IN-2

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₁₄F₂N₂O₂

[ Molecular Weight ]:
316.30

Tankyrase-IN-2

Names

Biological Activity

Chemical & Physical Properties

Related Compounds