Vevorisertib trihydrochloride
Modify Date: 2024-01-14 15:42:12
Vevorisertib trihydrochloride structure
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Common Name | Vevorisertib trihydrochloride | ||
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| 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 trihydrochlorideVevorisertib (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 |
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| 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 |
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| Molecular Weight | 696.11 |