Powder: -20°C for 3 years
In solvent: -80°C for 2 years
NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor.
Description | NVP-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] |
Synonyms | NVPTNKS656, Inhibitor, TNKS 656, PARP, inhibit, TNKS-656, TNKS656, Apoptosis, poly ADP ribose polymerase, NVP-TNKS-656, NVP TNKS656, NVP-TNKS656 |
Molecular Weight | 494.592 |
Formula | C27H34N4O5 |
CAS No. | 1419949-20-4 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 93 mg/mL (188 mM)
H2O: <1 mg/mL
Ethanol: 10 mg/mL(20.21 mM), warming
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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