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NVP-TNKS656, Wnt / Tankyrase Inhibitor

Overview
Catalog # bs-60328c-2-mg-solid
Product Name NVP-TNKS656, Wnt / Tankyrase Inhibitor
Specifications
Storage Buffer Powder
Storage Condition Store in dry, dark place at -20C for 1 year.
Target
Product Information Molecular Weight: 494.58

Formula: C27 H34 N4 O5

CAS Number: 1419949-20-4

InChi Key: DYGBNAYFDZEYBA-UHFFFAOYSA-N

InChi: InChI=1S/C27H34N4O5/c1-35-21-6-4-19(5-7-21)26(33)20-8-11-30(12-9-20)16-25(32)31(14-18-2-3-18)15-24-28-23-10-13-36-17-22(23)27(34)29-24/h4-7,18,20H,2-3,8-17H2,1H3,(H,28,29,34)

Smiles: COC1=CC=C(C=C1)C(=O)C1CCN(CC(=O)N(CC2NC(=O)C3COCCC=3N=2)CC2CC2)CC1

Purity: 98.0

Solubility: DMSO up to 100 mM; EtOH up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years
Description NVP-TNKS656 is a highly potent, selective and oral bioavailable tankyrase inhibitor with IC50 of 6 nM for TNKS2. It has 300-fold selectivity against PARP1 and PARP2. In MMTV-Wnt1 tumor models, NVP-TNKS656 was dosed to mice orally to stabilize Axin1 protein and reduce the Wnt/beta-catenin target gene Axin2 mRNA level by 70-80%. In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth.