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Vevorisertib

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Vevorisertib

Catalog No. T38847Cas No. 1416775-46-6

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].

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Pack Size	Price	Availability	Quantity
5 mg	$970	1-2 weeks

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Product Introduction

Bioactivity

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].
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].
Alias	Vevorisertib, ARQ 751

Chemical Properties

Molecular Weight	586.744
Formula	C35H38N8O
Cas No.	1416775-46-6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

ARQ751ARQ-751