STF 118804

STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.IC50 value:Target: NAMPT inhibitorin vitro: improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia, and targets leukemia stem cells. STF-118804 displays distinctive cytotoxicity by inducing apoptosis without causing a phase-specific cell cycle arrest. Over-expression of NAMPT rendered 293T cells more resistant to STF-118804 resulting in a higher IC50 (106 nM, 95% CI 74–151 nM) compared to control cells (17 nM, 95% CI 13–23 nM), further confirming that NAMPT protein levels dictate sensitivity to STF-118804 [1].in vivo: STF-118804 displayed high efficacy in a xenograft model of ALL. Mice treated with STF-118804 over a 20-day period survived an average of 34 days longer than vehicle-treated animals. During treatment, bioimaging showed regression of tumor followed by suppression of disease. STF-118804 was tolerated in the efficacious dose range, and the absence of adverse physical or pathological effects indicated that toxicity was not limiting in a 20-day study of mock transplanted mice [1].

Signaling Pathways >> Metabolic Enzyme/Protease >> Nampt

Research Areas >> Cancer

[1]. Matheny CJ, et al. Next-generation NAMPT inhibitors identified by sequential high-throughput phenotypic chemical and functional genomic screens. Chem Biol. 2013 Nov 21;20(11):1352-63.

FK866 (APO866, Daporinad) | P7C3 | GMX1778 | KPT-9274 | GNE-617 | Nampt-IN-1 | CB 300919 | CB30865