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NVP-TNKS656
- TNKS 656
- Soluble in DMSO
- MF: C27H34N4O5
- MW: 494.58
Description
Highly potent, selective and orally active tankyrase inhibitor and antagonist of Wnt pathway activity in the MMTV-Wnt1 mouse xenograft model (IC50 values 0.0155 µM and 0.0060 µM for TNKS1 and TNKS2, respectively and >5000-fold selectivity over PARP1 and PARP2).
More Information
| Parent CAS No. | 1419949-20-4 |
|---|---|
| Chemical Name | N-(cyclopropylmethyl)-2-(4-(4-methoxybenzoyl)piperidin-1-yl)-N-((4-oxo-4,5,7,8-tetrahydro-3H-pyrano[4,3-d]pyrimidin-2-yl)methyl)acetamide |
| SMILES | N1(CC(N(CC2CC2)CC2NC(=O)C3COCCC=3N=2)=O)CCC(C(=O)C2=CC=C(OC)C=C2)CC1 |
| MFCD | N.A. |
| InChi | InChI=1S/C27H34N4O5/c1-35-21-6-4-19(5-7-21)26(33)20-8-11-30(12-9-20)16-25(32)31(14-18-2-3-18)15-24-28-23-10-13-36-17-22(23)27(34)29-24/h4-7,18,20H,2-3,8-17H2,1H3,(H,28,29,34) |
| InChiKey | DYGBNAYFDZEYBA-UHFFFAOYSA-N |
| CID | 136237316 |
| Short Description | Wnt/TNKS inhibitor |
References
- MD Shultz et al. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor. J Med Chem. 2013 Aug 22;56(16):6495-511.
- M Schoumacher et al. Inhibiting Tankyrases sensitizes KRAS-mutant cancer cells to MEK inhibitors via FGFR2 feedback signaling. Cancer Res. 2014 Jun 15;74(12):3294-305.
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