1416775-08-0
1416775-08-0 structure
- Name: Vevorisertib trihydrochloride
- Chemical Name: Vevorisertib trihydrochloride
- CAS Number: 1416775-08-0
- Molecular Formula: C35H41Cl3N8O
- Molecular Weight: 696.11
- Catalog: Signaling Pathways PI3K/Akt/mTOR Akt
- Create Date: 2022-01-11 17:44:05
- Modify Date: 2024-01-14 15:42:12
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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]. |
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| 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]. [3]. Abstract A034: The use of biomarkers and ctDNA in a phase 1 trial of ARQ 751 |
| Molecular Formula | C35H41Cl3N8O |
|---|---|
| Molecular Weight | 696.11 |