Name | NVP-TNKS656 |
Description | NVP-TNKS656 (TNKS656) is a highly potent, selective, and orally active TNKS2 inhibitor. |
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] |
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.
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Keywords | NVPTNKS656 | Inhibitor | PARP | inhibit | Apoptosis | poly ADP ribose polymerase | NVP TNKS656 | NVP-TNKS-656 | NVP-TNKS 656 | TNKS-656 | TNKS 656 | NVP-TNKS656 |
Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Epigenetics Compound Library | Anti-Breast Cancer Compound Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Prostate Cancer Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Wnt/Hedgehog/Notch Compound Library |