1416775-46-6
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
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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 |
[3]. Abstract A034: The use of biomarkers and ctDNA in a phase 1 trial of ARQ 751 |
| Molecular Formula | C35H38N8O |
|---|---|
| Molecular Weight | 586.73 |