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Vevorisertib

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Catalog No. T38847Cas No. 1416775-46-6
Alias Vevorisertib, ARQ 751

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].

Vevorisertib
Other Forms of Vevorisertib:
Vevorisertib trihydrochlorideT388461416775-08-0
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Vevorisertib

😃Good
Catalog No. T38847Alias Vevorisertib, ARQ 751Cas 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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5 mg$9701-2 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].
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].
AliasVevorisertib, ARQ 751
Chemical Properties
Molecular Weight586.744
FormulaC35H38N8O
Cas No.1416775-46-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Keywords

ARQ751ARQ-751
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