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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $38 | In Stock | |
2 mg | $52 | In Stock | |
5 mg | $81 | In Stock | |
10 mg | $131 | In Stock | |
25 mg | $275 | In Stock | |
50 mg | $468 | In Stock | |
100 mg | $686 | In Stock | |
1 mL x 10 mM (in DMSO) | $89 | In Stock |
Description | NVP-TNKS656 (TNKS656) is a highly potent, selective, and orally active TNKS2 inhibitor. |
Targets&IC50 | TNKS2:6 nM |
In vitro | In vitro, NVP-TNKS656 shows low to moderate microsomal ER values across species and high solubility. [1] In PI3K or AKT inhibitor-resistant cells, NVP-TNKS656 blocks Wnt/β-Catenin pathway and promotes apoptosis. [2] |
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%. [1] In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth. [2] |
Alias | TNKS656 |
Molecular Weight | 494.58 |
Formula | C27H34N4O5 |
Cas No. | 1419949-20-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 93 mg/mL (188 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 10 mg/mL (20.21 mM), Heating is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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