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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-NAMPT-GNE-618
GNE-618

Chemical Structure : GNE-618

CAS No.: 1362151-42-5

GNE-618 (GNE618)

货号: PC-38787Not For Human Use, Lab Use Only.

GNE-618 is a potent, selective NAMPT inhibitor with IC50 of 6 nM, depletes NAD and induces cell death in vitro and in vivo.

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

生物&药学活性

GNE-618 is a potent, selective NAMPT inhibitor with IC50 of 6 nM, depletes NAD and induces cell death in vitro and in vivo.
GNE-618 reduced levels of NAD with an 50% minimal response (EC50) of 2.6 nM in the NSCLC cell line Calu-6, reduced cellular proliferation of Calu-6 cells with IC50 of 13. 6 nM.
NAMPT, but not NAPRT1, mRNA and protein levels inversely correlate with sensitivity to GNE-618 across a panel of 53 non-small cell lung carcinoma cell lines.
GNE-618 inhibits in vivo tumor growth in an A549 non-small cell lung carcinoma (NSCLC) model.

物理化学性质&存储条件

分子量 460.43
分子式 C21H15F3N4O3S
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-[[4-[[3-(Trifluoromethyl)phenyl]sulfonyl]phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide

参考文献

1. O'Brien T, et al. Neoplasia. 2013 Dec;15(12):1314-29.

2. Xiao Y, et al. Neoplasia. 2013 Oct;15(10):1151-60.

3. Zheng X, et al. J Med Chem 2013;56:6413–33.

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