product name NVP-TNKS656
Description: NVP-TNKS656, also known as TNKS656, is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2. 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.
References: J Med Chem. 2013 Aug 22;56(16):6495-511; Clin Cancer Res. 2016 Feb 1;22(3):644-56
494.58
Formula
C27H34N4O5
CAS No.
1419949-20-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (202.2 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (20.2 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | Athymic female nude mice bearing MMTV-Wnt1 tumors |
| Formulation & Dosage | Dissolved in 4% HCl:10% propylene glycol:20% Solutol HS15:60.5% D5W:0.5% NaOH; 350 mg/kg; Oral administration |
| References | J Med Chem. 2013 Aug 22;56(16):6495-511; Clin Cancer Res. 2016 Feb 1;22(3):644-56 |
