Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vevorisertib (ARQ 751) is a highly effective oral compound that selectively inhibits pan-AKT serine/threonine kinases such as AKT1 (with an IC50 value of 0.55 nM), AKT2 (with an IC50 value of 0.81 nM), and AKT3 (with an IC50 value of 1.31 nM). This compound, either as a standalone treatment option or in combination with other anti-cancer agents, is ideally suited for conducting research on solid tumors characterized by PIK3CA/AKT/PTEN mutations[4].
Pack Size | Availability | Price/USD | Quantity |
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5 mg | Inquiry | $ 970.00 |
Description | Vevorisertib (ARQ 751) is a highly effective oral compound that selectively inhibits pan-AKT serine/threonine kinases such as AKT1 (with an IC50 value of 0.55 nM), AKT2 (with an IC50 value of 0.81 nM), and AKT3 (with an IC50 value of 1.31 nM). This compound, either as a standalone treatment option or in combination with other anti-cancer agents, is ideally suited for conducting research on solid tumors characterized by PIK3CA/AKT/PTEN mutations[4]. |
Targets&IC50 | Akt3:1.31 nM (IC50), Akt2:0.81 nM (IC50), Akt1:0.55 nM (IC50) |
In vitro | Vevorisertib effectively targets and binds to both the wild-type AKT1 and its mutant form, AKT1-E17K, demonstrating high affinity with dissociation constants (K d) of 1.2 nM and 8.6 nM, respectively. Moreover, it inhibits the phosphorylation of pAKT(S473) in 293T cells that have been transiently transfected with AKT1-E17K[4]. |
In vivo | Vevorisertib, administered at doses ranging from 10 to 120 mg/kg, demonstrates a dose-dependent anti-tumor effect in a patient-derived xenograft (PDX) model of endometrial cancer characterized by the AKT1-E17K mutation. It exhibits a plasma half-life between 4 and 5 hours, with no observable accumulation in tissues[4]. |
Synonyms | Vevorisertib, ARQ 751 |
Molecular Weight | 586.744 |
Formula | C35H38N8O |
CAS No. | 1416775-46-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Vevorisertib 1416775-46-6 ARQ751 ARQ 751 ARQ-751 inhibitor inhibit