Vevorisertib trihydrochloride

Modify Date: 2024-01-14 15:42:12

Vevorisertib trihydrochloride structure	Common Name	Vevorisertib trihydrochloride
	CAS Number	1416775-08-0	Molecular Weight	696.11
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₃₅H₄₁Cl₃N₈O	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Vevorisertib trihydrochloride

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].

Name	Vevorisertib trihydrochloride

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

Molecular Formula	C₃₅H₄₁Cl₃N₈O
Molecular Weight	696.11

Vevorisertib trihydrochloride

Use of Vevorisertib trihydrochloride

Names

Vevorisertib trihydrochloride Biological Activity

Chemical & Physical Properties