| CAS NO: | 1419949-20-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 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) | Chemical Name: N-(cyclopropylmethyl)-2-(4-(4-methoxybenzoyl)piperidin-1-yl)-N-((4-oxo-4,5,7,8-tetrahydro-3H-pyrano[4,3-d]pyrimidin-2-yl)methyl)acetamide SMILES Code: O=C1NC(CN(CC2CC2)C(CN3CCC(C(C4=CC=C(OC)C=C4)=O)CC3)=O)=NC5=C1COCC5 |
| Synonyms | NVPTNKS-656; TNKS-656; NVP-TNKS656; TNKS 656; NVP-TNKS 656; TNKS656 |
| 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: NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is> 300 fold selectivity against PARP1 and PARP2. |
|---|---|
| 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 |
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