| Identification | Back Directory | [Name]
GNE 617 | [CAS]
1362154-70-8 | [Synonyms]
GNE617
GNE-617
GNE 617
CS-1587
GNE617;GNE 617
GNE-617 (CAS 1362154-70-8)
N-(4-((3,5-difluorophenyl)sulfonyl)benzyl)imidazo[1,2-a]pyridine-6-carboxamide
N-[[4-[(3,5-Difluorophenyl)sulfonyl]phenyl]methyl]imidazo[1,2-a]pyridine-6-carboxamide
Imidazo[1,2-a]pyridine-6-carboxamide, N-[[4-[(3,5-difluorophenyl)sulfonyl]phenyl]methyl]- | [Molecular Formula]
C21H15F2N3O3S | [MDL Number]
MFCD26960964 | [MOL File]
1362154-70-8.mol | [Molecular Weight]
427.42 |
| Chemical Properties | Back Directory | [density ]
1.42±0.1 g/cm3(Predicted) | [solubility ]
DMF:20.0(Max Conc. mg/mL);46.79(Max Conc. mM)
DMSO:78.67(Max Conc. mg/mL);26.22(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.47(Max Conc. mM) | [form ]
Powder | [pka]
11.69±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer. | [in vivo]
In rats, GNE-617 (administered QD) and GNE-875 (administered BID) are associated with more severe retinal toxicity at similar exposures and dosing duration compared with GMX-1778 (administered BID). The mouse efficacy studies using GNE-617, GNE-618, and GMX-1778 are designed to assess efficacy and opportunistically used to assess retinal toxicity in mice. NAMPTi retinal toxicity is observed with GNE-617 and GMX-1778; however, the different study durations between GNE-617 and GMX-1778 do not allow for direct comparison of retinal toxicity[2]. | [References]
[1] Shames DS, 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. DOI:10.1158/1078-0432.CCR-13-1186
[2] Zabka TS, et al. Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase. Toxicol Sci. 2015 Mar;144(1):163-72. DOI:10.1093/toxsci/kfu268 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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