This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
Miransertib (ARQ 092) HCl
Catalog No. T22247 CAS
1313883-00-9
Miransertib hydrochloride (ARQ-092 hydrochloride) is a powerful, orally bioavailable, selective, and allosteric inhibitor of Akt. It exhibits an inhibitory concentration (IC50) of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. In addition to its Akt inhibitory activity, Miransertib hydrochloride also demonstrates significant potency as an inhibitor of the AKT1-E17K mutant protein. This compound shows promise in research related to PI3K/AKT-driven tumors and Proteus syndrome. Furthermore, Miransertib hydrochloride displays efficacy against Leishmania [1, 2].
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Miransertib hydrochloride (ARQ-092 hydrochloride) is a powerful, orally bioavailable, selective, and allosteric inhibitor of Akt. It exhibits an inhibitory concentration (IC50) of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. In addition to its Akt inhibitory activity, Miransertib hydrochloride also demonstrates significant potency as an inhibitor of the AKT1-E17K mutant protein. This compound shows promise in research related to PI3K/AKT-driven tumors and Proteus syndrome. Furthermore, Miransertib hydrochloride displays efficacy against Leishmania [1, 2].
In vitro
In a comprehensive study involving various tumor-derived cell lines, Miransertib (ARQ-092; Compound 21a) demonstrated significant anti-proliferative effects in cell lines harboring mutations in PIK3CA/PIK3R1 compared to those with the wild-type (wt) PIK3CA/PIK3R1 or PTEN deficiency. Additionally, Miransertib effectively inhibited p-Akt (S473) and p-Akt (T308) in AN3CA and A2780 cells and suppressed p-PRAS40 (T246) with an IC 50 of 0.31 μM. Notably, Miransertib was highly effective against intracellular amastigotes of L. donovani or L. amazonensis in infected macrophages and promoted mTOR-dependent autophagy in Leishmania-infected macrophages, highlighting its diverse therapeutic potential.
In vivo
Miransertib (ARQ-092; Compound 21a) demonstrates effective oral bioavailability in rats (5 mg/kg) and monkeys (10 mg/kg), achieving absorption rates of 62% and 49%, respectively. In rats, it exhibits a half-life of 17 hours, longer than the 7 hours observed in monkeys. Concentration peaks reach 198 ng/mL in rats and 258 ng/mL in monkeys, with area under the curve (AUC) values recorded at 5496 h ng/mL and 2960 h ng/mL for each species. Additionally, Miransertib has been shown to effectively inhibit tumor growth in a human xenograft mouse model of endometrial adenocarcinoma [1].
Molecular Weight
468.98
Formula
C27H25ClN6
CAS No.
1313883-00-9
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.