Miransertib hydrochloride (Synonyms: ARQ-092 hydrochloride)

Name: Miransertib hydrochloride
Brand: MedChemExpress
SKU: HY-19719A
Rating: 5.0 (17 reviews)

Cat. No.: HY-19719A Purity: 99.74%: Data Sheet
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Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC₅₀s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib hydrochloride is effective against Leishmania.

For research use only. We do not sell to patients.

CAS No. : 1313883-00-9

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Miransertib hydrochloride:

Miransertib In-stock

17 Publications Citing Use of MCE Miransertib hydrochloride

In Vivo Imaging

: Miransertib hydrochloride purchased from MedChemExpress. Usage Cited in: Invest Ophthalmol Vis Sci. 2025 Aug 1;66(11):61. [Abstract]; Inhibition of ERK1/2 and Akt pathways by subconjunctival injection of the ERK1/2 inhibitor ravoxertinib hydrochloride and the Akt inhibitor Miransertib (270 µM, 5 µL/eye) reversed the role of PDGF-BB in promoting diabetic epithelial wound healing.

: Miransertib hydrochloride purchased from MedChemExpress. Usage Cited in: Invest Ophthalmol Vis Sci. 2025 Aug 1;66(11):61. [Abstract]; Inhibition of ERK1/2 and Akt pathways by subconjunctival injection of the ERK1/2 inhibitor ravoxertinib hydrochloride and the Akt inhibitor Miransertib (270 µM, 5 µL/eye) reversed the role of PDGF-BB in promoting diabetic epithelial nerve regeneration.

: Miransertib hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Pharm. 2025 Sep 1;22(9):5523-5532. [Abstract]; Immunoblots indicated the expression of proteins from cell extracts of H358 and H358R cells that were treated with DMSO or Miransertib (10 μM) for 48 h.

: Miransertib hydrochloride purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2024 Aug 13:284:116854. [Abstract]; Miransertib (1 µM) significantly blocked hesperetin’s ability to alleviate ferritin autophagy induced by AFB1. The decreased expression of FTL and ferritin, along with elevated levels of LC3B, provided evidence for this hypothesis.

: Miransertib hydrochloride purchased from MedChemExpress. Usage Cited in: FASEB J. 2022 Aug;36(8):e22423. [Abstract]; AKT and GSK3β signaling was suppressed by ARQ 092 (1 μM), and phosphorylated GSK3β was activated by AR 014418 in BMDMs afterforce application.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC₅₀s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research^[1]. Miransertib hydrochloride is effective against Leishmania^[2].

IC₅₀ & Target^[1]^[2]

Akt1

2.7 nM (IC₅₀)

Leishmania

Akt3

8.1 nM (IC₅₀)

Akt2

174 nM (IC₅₀)

Akt1 E17K mutant

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.73 μM Compound: 21a	Antiproliferative activity against human A2780 cells after 72 hrs by MTS/PMS assay Antiproliferative activity against human A2780 cells after 72 hrs by MTS/PMS assay	[PMID: 27305487]
AN3-CA	IC₅₀	0.71 μM Compound: 21a	Antiproliferative activity against human AN3CA cells after 72 hrs by MTS/PMS assay Antiproliferative activity against human AN3CA cells after 72 hrs by MTS/PMS assay	[PMID: 27305487]
IGROV-1	IC₅₀	0.21 μM Compound: 21a	Antiproliferative activity against human IGROV1 cells after 72 hrs by MTS/PMS assay Antiproliferative activity against human IGROV1 cells after 72 hrs by MTS/PMS assay	[PMID: 27305487]
LNCaP	IC₅₀	0.9 μM Compound: 21a	Antiproliferative activity against human LNCAP cells after 72 hrs by MTS/PMS assay Antiproliferative activity against human LNCAP cells after 72 hrs by MTS/PMS assay	[PMID: 27305487]
Sf9	IC₅₀	0.0027 μM Compound: 21a	Inhibition of full length unphosphorylated AKT1 (1 to 480 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by Alphascreen assay Inhibition of full length unphosphorylated AKT1 (1 to 480 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by Alphascreen assay	[PMID: 27305487]
Sf9	IC₅₀	0.0045 μM Compound: 21a	Inhibition of full length active AKT2 (1 to 481 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate/PDK1/MAPKAPK2/DOPS/DOPC/PtdIns(3,4,5)P3 addition measured after 30 mins by Alphascreen assay Inhibition of full length active AKT2 (1 to 481 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate/PDK1/MAPKAPK2/DOPS/DOPC/PtdIns(3,4,5)P3 addition measured after 30 mins by Alphascreen assay	[PMID: 27305487]
Sf9	IC₅₀	0.005 μM Compound: 21a	Inhibition of full length active AKT1 (1 to 480 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate/PDK1/MAPKAPK2/DOPS/DOPC/PtdIns(3,4,5)P3 addition measured after 30 mins by Alphascreen assay Inhibition of full length active AKT1 (1 to 480 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate/PDK1/MAPKAPK2/DOPS/DOPC/PtdIns(3,4,5)P3 addition measured after 30 mins by Alphascreen assay	[PMID: 27305487]
Sf9	IC₅₀	0.0081 μM Compound: 21a	Inhibition of full length unphosphorylated AKT3 (1 to 479 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by Alphascreen assay Inhibition of full length unphosphorylated AKT3 (1 to 479 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by Alphascreen assay	[PMID: 27305487]
Sf9	IC₅₀	0.014 μM Compound: 21a	Inhibition of full length unphosphorylated AKT2 (1 to 481 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by Alphascreen assay Inhibition of full length unphosphorylated AKT2 (1 to 481 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by Alphascreen assay	[PMID: 27305487]
Sf9	IC₅₀	0.016 μM Compound: 21a	Inhibition of full length active AKT3 (1 to 479 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate/PDK1/MAPKAPK2/DOPS/DOPC/PtdIns(3,4,5)P3 addition measured after 30 mins by Alphascreen assay Inhibition of full length active AKT3 (1 to 479 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate/PDK1/MAPKAPK2/DOPS/DOPC/PtdIns(3,4,5)P3 addition measured after 30 mins by Alphascreen assay	[PMID: 27305487]

In Vitro

In a large panel of cell lines derived from various tumor types, Miransertib (ARQ-092; Compound 21a) shows potent anti-proliferative activity in cell lines containing PIK3CA/PIK3R1 mutations compared to those with wild-type (wt) PIK3CA/PIK3R1 or PTEN loss. Miransertib shows excellent inhibition of p-Akt (S473) and p-Akt (T308) in both AN3CA and A2780 cells. The inhibition of the downstream protein p-PRAS40 (T246) is observed with Miransertib (IC₅₀=0.31 μM)^[1].
Miransertib is markedly effective against intracellular amastigotes of L. donovani or L. amazonensis-infected macrophages. Miransertib also enhances mTOR dependent autophagy in Leishmania-infected macrophages^[2]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Miransertib (ARQ-092; Compound 21a) shows good absolute oral bioavailability in rats (5 mg/kg) and monkeys (10 mg/kg) with F values of 62% and 49%, respectively. The half-life is longer in rats compared to monkeys with t_1/2 values of 17 h in rats versus 7 h in monkeys. The C_max is 198 ng/mL and 258 ng/mL and the AUC_inf was 5496 h•ng/mL and 2960 h•ng/mL in rats and monkeys, respectively^[1].
Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

468.98

Formula

C₂₇H₂₅ClN₆

CAS No.

1313883-00-9

Appearance

Solid

Color

Light yellow to brown

SMILES

NC1=NC=CC=C1C2=NC3=CC=C(C4=CC=CC=C4)N=C3N2C5=CC=C(C6(N)CCC6)C=C5.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (106.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1323 mL	10.6614 mL	21.3229 mL
5 mM	0.4265 mL	2.1323 mL	4.2646 mL
10 mM	0.2132 mL	1.0661 mL	2.1323 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.74%

Select Batch:

Data Sheet (294 KB) SDS (393 KB)

COA (259 KB)

Handling Instructions (2659 KB)

References

[1]. Lapierre JM, et al. Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor. J Med Chem. 2016 Jul 14;59(13):6455-69. [Content Brief]

[2]. Devki Nandan, et al. Miransertib (ARQ 092), an orally-available, selective Akt inhibitor is effective against Leishmania. PLoS One. 2018 Nov 6;13(11):e0206920. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1323 mL	10.6614 mL	21.3229 mL	53.3072 mL
	5 mM	0.4265 mL	2.1323 mL	4.2646 mL	10.6614 mL
	10 mM	0.2132 mL	1.0661 mL	2.1323 mL	5.3307 mL
	15 mM	0.1422 mL	0.7108 mL	1.4215 mL	3.5538 mL
	20 mM	0.1066 mL	0.5331 mL	1.0661 mL	2.6654 mL
	25 mM	0.0853 mL	0.4265 mL	0.8529 mL	2.1323 mL
	30 mM	0.0711 mL	0.3554 mL	0.7108 mL	1.7769 mL
	40 mM	0.0533 mL	0.2665 mL	0.5331 mL	1.3327 mL
	50 mM	0.0426 mL	0.2132 mL	0.4265 mL	1.0661 mL
	60 mM	0.0355 mL	0.1777 mL	0.3554 mL	0.8885 mL
	80 mM	0.0267 mL	0.1333 mL	0.2665 mL	0.6663 mL
	100 mM	0.0213 mL	0.1066 mL	0.2132 mL	0.5331 mL

Miransertib hydrochloride Related Classifications

Help & FAQs

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Miransertib hydrochloride (Synonyms: ARQ-092 hydrochloride)

Customer Review

Other Forms of Miransertib hydrochloride:

17 Publications Citing Use of MCE Miransertib hydrochloride

Featured Recommendations

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View All Akt Isoform Specific Products:

View All Parasite Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

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Complete Stock Solution Preparation Table

Miransertib hydrochloride Related Classifications

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Miransertib hydrochloride (Synonyms: ARQ-092 hydrochloride)

Customer Review

Other Forms of Miransertib hydrochloride:

Miransertib hydrochloride Related Antibodies

17 Publications Citing Use of MCE Miransertib hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Akt Isoform Specific Products:

View All Parasite Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Miransertib hydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Miransertib hydrochloride Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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