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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-NVP-TNKS656
NVP-TNKS656

Chemical Structure : NVP-TNKS656

CAS No.: 1419949-20-4

NVP-TNKS656 (TNKS656)

货号: 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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 494.59
分子式 C27H34N4O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

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

参考文献

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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