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CAS No.: 1362154-70-8

GNE-617 Catalog No. CSN17752

Synonyms: GNE-617

GNE-617 is a potent NAMPT inhibitor with IC50 value of 5nM.

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400-920-2911

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技术信息

生物活性

描述Nicotinamide adenine dinucleotide (NAD) is an important biomolecule implicated in a large number of cellular processes ranging from cell metabolism and survival to calcium homeostasis. Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the first and rate-determining step of recycling nicotinamide (NAM) back to NAD. Blockade of the NAM-NAD recycling pathway via NAMPT inhibition might be an appropriate therapeutic strategy for oncology indications ^[3]. GNE-617 inhibits human NAMPT in a biochemical assay with an IC₅₀ of 5 nM and reduces NAD levels across a panel of six diverse cancer cell lines with a t_1/2 of NAD reduction ranging from 6.5 to 12.5 h. NAD depletion caused by GNE-617 results in cell death, with an observed increase in a sub2N population. Cell growth was attenuated within 32–40 h in A549, Calu6, HCT116, and PC-3 cells following treatment with 200 nM GNE-617 for 138 h. To measure cell motility, the change in location for 100 individual cells was tracked hourly for 102 h following exposure to 200 nM GNE-617. Control A549 and Calu6 cells displayed an average motility of 15.1 ± 1.7 and 10.2 ± 1.1 μM per hour, respectively, whereas cells exposed to GNE-617 showed a decrease in motility starting as early as 21 h, corresponding to the case when NAD levels have decreased by 95% ^[4].
参考文献

[1] Zabka TS, Singh J, et al. Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase. Toxicol Sci. 2015 Mar;144(1):163-72.
[2] Shames DS, Elkins K, et al. Loss of NAPRT1 expression by tumor-specific promoter methylation provides a novel predictive biomarker for NAMPT inhibitors. Clin Cancer Res. 2013 Dec 15;19(24):6912-23.
[3] Zak M, Liederer BM, Sampath D, Yuen PW, Bair KW, Baumeister T, Buckmelter AJ, Clodfelter KH, Cheng E, Crocker L, Fu B, Han B, Li G, Ho YC, Lin J, Liu X, Ly J, O'Brien T, Reynolds DJ, Skelton N, Smith CC, Tay S, Wang W, Wang Z, Xiao Y, Zhang L, Zhao G, Zheng X, Dragovich PS. Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility. Bioorg Med Chem Lett. 2015 Feb 1;25(3):529-41. doi: 10.1016/j.bmcl.2014.12.026. Epub 2014 Dec 17. PMID: 25556090.
[4] Del Nagro C, Xiao Y, Rangell L, Reichelt M, O'Brien T. Depletion of the central metabolite NAD leads to oncosis-mediated cell death. J Biol Chem. 2014 Dec 19;289(51):35182-92. doi: 10.1074/jbc.M114.580159. Epub 2014 Oct 29. PMID: 25355314; PMCID: PMC4271207.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3396 mL
- 11.6980 mL
- 23.3960 mL
- 5 mM
- 0.4679 mL
- 2.3396 mL
- 4.6792 mL
- 10 mM
- 0.2340 mL
- 1.1698 mL
- 2.3396 mL

技术信息

CAS号

1362154-70-8

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H15F2N3O3S

运输

蓝冰

分子量

427.42

别名

GNE-617

溶解度

DMSO	42.0 mg/mL (98.3 mM)
Water	Insoluble
Ethanol	Insoluble

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