Tankyrase-IN-2

Modify Date: 2024-01-15 12:05:50

Tankyrase-IN-2 structure	Common Name	Tankyrase-IN-2
	CAS Number	1588870-36-3	Molecular Weight	316.30
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₇H₁₄F₂N₂O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Tankyrase-IN-2

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

Tankyrase-IN-2

Use of Tankyrase-IN-2

Names

Tankyrase-IN-2 Biological Activity

Chemical & Physical Properties