Vevorisertib

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Vevorisertib

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1416775-46-6

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

ARQ 751

产品介绍

Vevorisertib (ARQ 751) 是一种具有口服活性、有效和选择性的pan-AKT丝氨酸/苏氨酸激酶抑制剂，对AKT1(IC₅₀=0.55 nM)、AKT2(IC₅₀=0.81 nM) 和AKT3(IC₅₀=1.31 nM) 有抑制作用。Vevorisertib 单体化合物或与其他抗癌化合物联用，可用于 PIK3CA/AKT/PTEN 突变的实体瘤研究。

生物活性

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].

IC₅₀& Target^[4]

Akt1

0.55 nM (IC₅₀)

Akt2

0.81 nM (IC₅₀)

Akt3

1.31 nM (IC₅₀)

体外研究
(In Vitro)

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].

体内研究
(In Vivo)

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].

Clinical Trial

分子量

586.73

Formula

C₃₅H₃₈N₈O

CAS 号

1416775-46-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.