NAMPT/IDO1-IN-1 

NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC₅₀s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel^[1].

NAMPT/IDO1-IN-1 (compound 10e) (10 μM; 48 h) shows antiproliferative activity against A549/R cells in an NAMPT- and IDO1-dependent manner^[1].
NAMPT/IDO1-IN-1 (5 μM, 10 μM, 15 μM; 12 d) inhibits colony formation of A549/R cells and promotes the accumulation of intracellular ROS in a dose-dependent manner^[1].
NAMPT/IDO1-IN-1 (10 μM; 24 h) reduces NAD+ in A549/R cells in an NAMPT- and IDO1-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NAMPT/IDO1-IN-1 (compound 10e) (5 μM; 24 h) shows ROS-boosting effect in Zebrafish embryos, led to a level of ROS much higher than that of LPS (50 μg/mL)^[1].
NAMPT/IDO1-IN-1 (25 mg/kg; p.o.; single dose) has good p.o. bioavailability and (5 mg/kg; i.v.; single dose) displays moderate overall exposure^[1].
NAMPT/IDO1-IN-1 (50, 100, and 200 mg/kg; p.o.; twice daily for 3 weeks) also shows in vivo anti-tumor effect in an A549/R tumor xenograft model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

559.39

C₂₃H₂₄BrFN₈O₃

2247884-06-4

BrC(C=C1N/C(C2=NON=C2NCCCCCCNC(C3=CN4C(C=C3)=NC=C4)=O)=N\O)=C(C=C1)F

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wang K, et al. Dual Nicotinamide Phosphoribosyltransferase (NAMPT) and Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors for the Treatment of Drug-Resistant Nonsmall-Cell Lung Cancer. J Med Chem. 2023 Jan 12;66(1):1027-1047.  [Content Brief]