Vevorisertib trihydrochloride

Names

[ Name ]:
Vevorisertib trihydrochloride

Biological Activity

[Description]:

Vevorisertib (ARQ 751) (trihydrochloride) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib (trihydrochloride), as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations[1][2][3][4].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> PI3K/Akt/mTOR >> Akt

[Target]

Akt1:0.55 nM (IC50)

Akt2:0.81 nM (IC50)

Akt3:1.31 nM (IC50)

[In Vitro]

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

[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].

[References]

[1]. [1]. Vevorisertib (ARQ 751) (4440-001) as a Single Agent or in Combination With Other Anti-Cancer Agents, in Solid Tumors With PIK3CA / AKT / PTEN Mutations.

[2]. [2]. ArQule Presents Recent Data on ARQ 751 at the 2019 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics.

[3]. [3]. Abstract A034: The use of biomarkers and ctDNA in a phase 1 trial of ARQ 751

[4]. [4]. Abstract 374: In vitro and in vivo anti-tumor activity of ARQ 751, a potent and selective AKT inhibitor

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₅H₄₁Cl₃N₈O

[ Molecular Weight ]:
696.11

Vevorisertib trihydrochloride

Names

Biological Activity

Chemical & Physical Properties

Related Compounds