Vevorisertib (ARQ 751) is an orally active, potent and selectivepan-AKTserine/threonine kinaseinhibitor againstAKT1(IC₅₀=0.55 nM),AKT2(IC₅₀=0.81 nM), andAKT3(IC₅₀=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA /AKT/PTENmutations^[1][2][3][4].

Vevorisertib binds to wild-type AKT1 and mutant AKT1-E17K with K_dof 1.2 nM and 8.6 nM, respectively, and suppresses pAKT(S473) in 293T cells transiently transfected with AKT1-E17K^[4].

Vevorisertib (10~120 mg/kg) exerts dose-dependent anti-tumor activity in an AKT1-E17K mutant endometrial patient-derived xenograft (PDX) model. Vevorisertib shows a plasma half-life of 4 to 5 hours and no tissue accumulation^[4].

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C₃₅H₃₈N₈O

1416775-46-6

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