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Chemical Structure : NVP-TNKS656
CAS No.: 1419949-20-4
Catalog No.: PC-49490Not For Human Use, Lab Use Only.
NVP-TNKS656 (TNKS656) is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM (TNKS2), 5,000-fold selectivity versus PARP1 and PARP2.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $78 | In stock | |
| 10 mg | $118 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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NVP-TNKS656 (TNKS656) is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM (TNKS2), 5,000-fold selectivity versus PARP1 and PARP2.
NVP-TNKS656 shows high potency in HEK293 SuperTopFlash reporter gene assay with IC50 of 3.5 nM.
NVP-TNKS656 sensitizes KRAS-mutant cancer cells to MEK inhibitors via FGFR2 feedback signaling, dual inhibition of TNKS and MEK leads to more robust apoptosis and antitumor activity both in vitro and in vivo.
NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth in PI3K or AKT inhibitor-resistant cells.
| M.Wt | 494.59 | |
| Formula | C27H34N4O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-Cyclopropylmethyl-2-[4-(4-methoxybenzoyl)piperidin-1-yl]-N-[(4-oxo-4,5,7,8-tetrahydro-4H-pyrano[4,3-d]pyrimidin-2-yl)methyl]acetamide |
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1. Shultz MD, et al. J Med Chem. 2013 Aug 22;56(16):6495-511.
2. Arqués O, et al. Clin Cancer Res. 2016 Feb 1;22(3):644-56.
3. Schoumacher M, et al. Cancer Res. 2014 Jun 15;74(12):3294-305.
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