PD-L1/Nampt-IN-1 

PD-L1/Nampt-IN-1 is an orally active inhibitor that simultaneously target PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC₅₀s value of 63 nM and 582 nM. PD-L1/Nampt-IN-1 demonstrates cross-species affinity with comparable K_D values for hPD-L1 (52.6 nM) and mPD-L1 (49.1 nM), respectively. PD-L1/Nampt-IN-1 effectively inhibits tumor growth by activating the tumor immune microenvironment. PD-L1/Nampt-IN-1 can be used for the study of melanoma^[1].

PD-L1/Nampt-IN-1 (Compound T8) (0.5-5 μM) can enhance the inhibition of the PD-1/PD-L1 interaction in a dose-dependent manner and reachs 76.63% at 5 μM^[1].

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

PD-L1/Nampt-IN-1 (Compound T8) (50 mg/kg, p.o., for 14 days) achieves enhanced tumor growth inhibition in B16-F10 tumor mice model, mechanistically attributed to the activation of the tumor immune microenvironment^[1].
PD-L1/Nampt-IN-1 is highly concentrated in tumors (1133.6 ng/mL at 8 hours), and penetrates the blood-brain barrier (81.86 ng/mL at 1 hour)^[1].

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

452.55

C₂₈H₂₈N₄O₂

3054043-85-2

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• [1]. Lv J, Cheng B, Song C. Rational design of NAMPT-based dual inhibitors with improved drug-like and pharmacokinetic properties for cancer treatment. Eur J Med Chem. 2025 Nov 5;297:117966.  [Content Brief]