NVP-TNKS656 - TNKS 656

Based on 24 reference(s) in Google Scholar 8 10 24

Axon 2599

CAS [1419949-20-4]

MF C27H34N4O5
MW 494.58

Purity: 99%
Soluble in DMSO

NVP-TNKS656

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).

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.

Cell Cycle Regulation Cell Signaling & Oncology Stem Cell Wnt-β-Catenin DNA-damage Response EC 2.4.2.30 TNKS

Selective and orally active TNKS inhibitor and antagonist of Wnt pathway activity

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

Parent CAS No.

[1419949-20-4]

产品资料