NVP-TNKS656
Catalog No.S7238
Molecular Weight(MW): 494.58
NVP-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.
Purity & Quality Control
Choose Selective PARP Inhibitors
Biological Activity
| Description | NVP-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. |
|---|---|
| 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] |
Protocol
| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (202.19 mM) |
|---|---|---|
| Ethanol | 10 mg/mL warmed (20.21 mM) | |
| Water | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 494.58 |
|---|---|
| Formula | C27H34N4O5 |
| CAS No. | 1419949-20-4 |
| Storage | powder |
| Synonyms | N/A |
Bio Calculators
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