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1416775-46-6

1416775-46-6 structure
1416775-46-6 structure
  • Name: Vevorisertib
  • Chemical Name: Vevorisertib
  • CAS Number: 1416775-46-6
  • Molecular Formula: C35H38N8O
  • Molecular Weight: 586.73
  • Catalog: Signaling Pathways PI3K/Akt/mTOR Akt
  • Create Date: 2021-12-20 12:08:28
  • Modify Date: 2024-04-02 19:43:31
  • Vevorisertib (ARQ 751) 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, 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
Description Vevorisertib (ARQ 751) 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, 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
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]. 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]. ArQule Presents Recent Data on ARQ 751 at the 2019 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics.

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

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

Molecular Formula C35H38N8O
Molecular Weight 586.73