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Overview
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Background
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].
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- Properties
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Overview