Nampt-IN-19 

Nampt-IN-19 is an orally active and non-substrate nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with a human K_i of 5.6 nM. Nampt-IN-19 blocks NAD⁺ biosynthesis from Nicotinamide (HY-B0150). Nampt-IN-19 acts as an antiproliferative agent in cancer cells. Nampt-IN-19 has preclinical pharmacokinetic properties supporting oral antitumor activity in mouse xenograft models. Nampt-IN-19 can be used for the research of colorectal cancer^[1].

Nampt-IN-19 (52) binds to human NAMPT with a K_i of 5.6 nM^[1].
Nampt-IN-19 inhibits PC-3 human prostate cancer cell viability with an IC₅₀ of 24 nM^[1].
Nampt-IN-19 inhibits CYP3A4 with an IC₅₀ of 16 μM and CYP2C9 with an IC₅₀ of 8.4 μM^[1].
Nampt-IN-19 has a scaled unbound intrinsic clearance of <3.4 L/h/kg in rat microsomes^[1].
Nampt-IN-19 has a scaled unbound intrinsic clearance of 18 L/h/kg in mouse microsomes^[1].
Nampt-IN-19 has a scaled unbound intrinsic clearance of 3.5 L/h/kg in human microsomes^[1].

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

Nampt-IN-19 (52) (15 mg/kg/day; p.o.; 3 on, 4 off; for 21 days) has a TGI rate of 90% in a murine xenograft model using the HCT-116 cell line^[1].

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

421.53

C₂₅H₃₁N₃O₃

2109805-79-8

O=C(N1CC2=C(C1)C=CC=C2)NC3=CC=C(C4CCN(CC4)C(CC(C)(C)O)=O)C=C3

Room temperature in continental US; may vary elsewhere.

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

• [1]. Curtin ML, et al. SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT). Bioorg Med Chem Lett. 2017;27(15):3317-3325.  [Content Brief]