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. |