NVP-TNKS656

SKU: orb1304373

Description

NVP-TNKS656

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1419949-20-4
• MW: 494.58
• Purity: 96.79%
• Formula: C₂₇H₃₄N₄O₅
• SMILES: COc1ccc(cc1)C(=O)C1CCN(CC(=O)N(CC2CC2)Cc2nc3CCOCc3c(=O)[nH]2)CC1
• Target: Apoptosis,Wnt/beta-catenin,PARP
• Solubility: DMSO:93 mg/mL (188.04 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.67 mM);Ethanol:10 mg/mL (20.22 mM)

Bioactivity

• Target IC50:
  PARP2:32 μM|TNKS2:6 nM
• In Vivo:
  In mice, NVP-TNKS656 displays low clearance and volume of distribution, and exhibits good exposure and moderate oral bioavailability. In MMTV-Wnt1 tumor bearing athymic nude mice, NVP-TNKS656 (350 mg/kg, p.o.) stabilizes Axin1 protein and reduces 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.
• In Vitro:
  In vitro, NVP-TNKS656 shows low to moderate microsomal ER values across species and high solubility. In PI3K or AKT inhibitor-resistant cells, NVP-TNKS656 blocks Wnt/β-Catenin pathway and promotes apoptosis.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Wnt/β-catenin, Wnt/b-catenin, Wnt/betacatenin, Wnt, poly ADP ribose polymerase, TNKS 656, TNKS656, TNKS-656, TNKS2, βcatenin, beta-catenin, betacatenin, bcatenin, Apoptosis, Inhibitor, PARP, NVP TNKS656, NVP-TNKS 656, NVPTNKS656, NVP-TNKS656, NVP-TNKS-656, inhibit

Compound Identifiers

PubChem CID

136237316