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Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor with inhibitory effects on AKT1/AKT2/AKT3 and is commonly used in the study of solid tumors with PIK3CA/AKT/PTEN mutations, showing dose-dependent antitumor activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $162 | In Stock | |
5 mg | $396 | In Stock | |
10 mg | $752 | In Stock | |
25 mg | $1,650 | In Stock | |
50 mg | $2,620 | In Stock |
Description | Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor with inhibitory effects on AKT1/AKT2/AKT3 and is commonly used in the study of solid tumors with PIK3CA/AKT/PTEN mutations, showing dose-dependent antitumor activity. |
Targets&IC50 | Akt2:0.81 nM, Akt3:1.31 nM, Akt3:1.31 nM (IC50), Akt1:0.55 nM, Akt2:0.81 nM (IC50), Akt1:0.55 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 inhibits pAKT(S473) in 293T cells transiently transfected with AKT1-E17K.[4] |
In vivo | Vevorisertib (10-120 mg/kg) has dose-dependent antitumor activity in AKT1-E17K mutant endometrial patient xenograft (PDX) models.[4] |
Alias | ARQ751, ARQ 751 |
Molecular Weight | 586.73 |
Formula | C35H38N8O |
Cas No. | 1416775-46-6 |
Smiles | O=C(N(C)C1CCN(C2=CC=CC(=C2)C3=NC4=C(N=C(C5=CC=CN=C5N)N4C6=CC=C(C=C6)C7(N)CCC7)C=C3)CC1)C |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||
Solubility Information | DMSO: 4.00 mg/mL (6.82 mM), Sonication is recommended. | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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