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STF-118804
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
STF-118804图片
CAS NO:894187-61-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
50mg电议

产品介绍
STF-118804 是一种高度特异性的 NAMPT 抑制剂;降低大多数 B-ALL 细胞系的活力,IC50<10 nM。
Cas No.894187-61-2
别名烟酰胺磷酸核糖基转移酶
化学名4-[5-methyl-4-[(4-methylphenyl)sulfonylmethyl]-1,3-oxazol-2-yl]-N-(pyridin-3-ylmethyl)benzamide
Canonical SMILESCC1=CC=C(C=C1)S(=O)(=O)CC2=C(OC(=N2)C3=CC=C(C=C3)C(=O)NCC4=CN=CC=C4)C
分子式C25H23N3O4S
分子量461.53
溶解度≥ 19.1mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

STF-118804 is an inhibitor of NAMPT [1].

Nicotinamide phosphoribosyl transferase (NAMPT) is a rate-limiting enzyme in the biosynthesis of nicotinamide adenine dinucleotide (NAD+), an important cofactor in many biochemical and biological processes. Also, NAMPT is a cytokine that inhibits neutrophil apoptosis and promotes B cell maturation [1].

STF-118804 is a NAMPT inhibitor. In B-ALL cell lines, STF-118804 reduced the viability with high potency. In leukemic samples from pediatric acute lymphoblastic leukemia (ALL) patients, STF-118804 reduced the viability with IC50 values of 3.1-32.3 nM. In MV411 cells, STF-118804 induced apoptosis without cell cycle arrest. Also, STF-118804 showed high potency in colon and prostate cell lines. STF-118804 (10 μM) inhibited NAD+ production from nicotinamide. In 293T cells over-expressing NAMPT, STF-118804 reduced the viability with IC50 value of 106 nM. However, STF-118804 had no effect on cells over-expressing H191R or G217R mutants [1].

In mice bearing orthotopic xenograft model of ALL, STF-118804 increased survival and inhibited tumor growth. Also, STF-118804 effectively reduced leukemia stem cells [1].

Reference:
[1].  Matheny CJ, Wei MC, Bassik MC, et al. Next-generation NAMPT inhibitors identified by sequential high-throughput phenotypic chemical and functional genomic screens. Chem Biol, 2013, 20(11): 1352-1363.