GNE-495

1449277-10-4

C22H20FN5O2

DMSO : 2.17 mg/mL (5.35 mM; Need ultrasonic)

MAPK/ERK Pathway

GNE-495 is a potent and selective MAP4K4 inhibitor with an IC₅₀ of 3.7 nM. IC50 & Target: IC50: 3.7 nM (MAP4K4)^[1] In Vitro: GNE-495 is a potent and selective MAP4K4 inhibitor with efficacy in retinal angiogenesis. GNE-495 shows the best balance of MAP4K4 inhibition, permeability, microsomal stability, and cellular potency^[1]. In Vivo: GNE-495 is administered intraperitoneally to neonatal mouse pups at high doses: 25 and 50 mg/kg. GNE-495 shows good in vivo profile in all species tested, with low clearances, moderate terminal half-lives, and reasonable oral exposure levels (F=37-47%)^[1].