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Miransertib hydrochloride

Name: Miransertib hydrochloride
Brand: TargetMol
SKU: T22247
Price: 43 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T22247Cas No. 1313883-00-9

Alias Miransertib (ARQ 092) HCl, ARQ-092 hydrochloride

Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally bioavailable, selective, and allosteric inhibitor of Akt with an IC50 of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. It also shows significant potency against the AKT1-E17K mutant protein and holds promise for research on PI3K/AKT-driven tumors and Proteus syndrome. Additionally, Miransertib hydrochloride exhibits efficacy against Leishmania [1, 2].

Miransertib hydrochloride

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Purity: 99.81%

Catalog No. T22247Alias Miransertib (ARQ 092) HCl, ARQ-092 hydrochlorideCas No. 1313883-00-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$43	-	In Stock
5 mg	$94	-	In Stock
10 mg	$136	-	In Stock
25 mg	$225	-	In Stock
50 mg	$332	-	In Stock
100 mg	$493	-	In Stock
200 mg	$719	-	In Stock
1 mL x 10 mM (in DMSO)	$109	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.81%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally bioavailable, selective, and allosteric inhibitor of Akt with an IC50 of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. It also shows significant potency against the AKT1-E17K mutant protein and holds promise for research on PI3K/AKT-driven tumors and Proteus syndrome. Additionally, Miransertib hydrochloride exhibits efficacy against Leishmania [1, 2].
Targets&IC50	Akt2:174 nM, Akt1:2.7 nM, Akt3:8.1 nM
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 (62%, 5 mg/kg) and monkeys (49%, 10 mg/kg), with half-lives of 17 hours and 7 hours, respectively. Peak plasma concentrations are 198 ng/mL in rats and 258 ng/mL in monkeys, with AUC values of 5496 h·ng/mL and 2960 h·ng/mL, respectively. Additionally, Miransertib effectively inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma [1].
Synonyms	Miransertib (ARQ 092) HCl, ARQ-092 hydrochloride

Chemical Properties

Molecular Weight	468.98
Formula	C₂₇H₂₅ClN₆
Cas No.	1313883-00-9
Smiles	Cl.Nc1ncccc1-c1nc2ccc(nc2n1-c1ccc(cc1)C1(N)CCC1)-c1ccccc1
Relative Density.	no data available

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (85.29 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Saline: 2 mg/mL (4.26 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1323 mL	10.6614 mL	21.3229 mL	106.6144 mL
5 mM	0.4265 mL	2.1323 mL	4.2646 mL	21.3229 mL
10 mM	0.2132 mL	1.0661 mL	2.1323 mL	10.6614 mL
20 mM	0.1066 mL	0.5331 mL	1.0661 mL	5.3307 mL
50 mM	0.0426 mL	0.2132 mL	0.4265 mL	2.1323 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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