Nampt-IN-10 TFA

Nampt-IN-10 TFA (compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-10 TFA shows cellular potency to A2780 and CORL23 cells lines with IC50s of 5 and 19 nM, respectively. Nampt-IN-10 TFA can be used as a novel non-antimitotic payload for ADCs[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Nampt

IC50: 5 nM (A2780), 19 nM (CORL23), 2 nM (NCI-H526 with c-Kit expressing), 0.4 nM (MDA-MB453 with HER2 expressing), 1 nM (NCI-N87 with HER2 expressing)[1]

Nampt-IN-10 TFA (0-1 μM; 72 h) shows cellular potency to A2780, CORL23, and c-Kit and HER2 expressing cell lines[1]. Cell Cytotoxicity Assay[1] Cell Line: A2780, CORL23, NCI-H526 with c-Kit expressing, MDA-MB453 and NCI-N87 with HER2 expressing cell lines Concentration: 0-1 μM Incubation Time: 72 hours Result: Showed cellular potency towards A2780, CORL23, NCI-H526 with c-Kit expressing, MDA-MB453 and NCI-N87 with HER2 expressing cells with IC50 values of 5, 19, 2, 0.4 and 1 nM, respectively.

[1]. Karpov AS, et al. Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates. ACS Med Chem Lett. 2018 Jun 28;9(8):838-842.