| STF-118804NAMPT inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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| Cas No. | 894187-61-2 | SDF | Download SDF |
| Chemical Name | 4-[5-methyl-4-[(4-methylphenyl)sulfonylmethyl]-1,3-oxazol-2-yl]-N-(pyridin-3-ylmethyl)benzamide | ||
| Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)CC2=C(OC(=N2)C3=CC=C(C=C3)C(=O)NCC4=CN=CC=C4)C | ||
| Formula | C25H23N3O4S | M.Wt | 461.53 |
| Solubility | ≥19.1mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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