Art. -Nr.: HY-19719A

Miransertib hydrochloride

Name: Miransertib hydrochloride
Brand: MedChemExpress
SKU: HY-19719A
Price: 130.00 USD
Availability: InStock
Rating: 5 (21 reviews)

(Synonyms: ARQ-092 hydrochloride)

21 Cited Publications

Kundenbewertung

Based on 21 publication(s) in Google Scholar

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.

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Reinheit : 99.74%
CAS. Nr.: 1313883-00-9
Formel: C₂₇H₂₅ClN₆
Molecular Weight:468.98

Speicherung:

4°C, sealed storage, away from moisture

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

Miransertib hydrochloride Chemical Structure

CAS. Nr.: 1313883-00-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (21)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle Parasite Isoform-spezifische Produkte anzeigen :

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 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	[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 addi 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 addi	[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 addi 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 addi	[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 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	[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 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	[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 addi 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 addi	[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.

Chemical Information

CAS. Nr. 1313883-00-9
Appearance Solid
Molecular Weight 468.98
Formel C₂₇H₂₅ClN₆
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
Synonyms

ARQ-092 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Publications (21)

All WBIn Vivo Imaging

Sort by:

Journal Impact Factor

Signal Transduct Target Ther

Targeted therapy for capillary-venous malformations. [Abstract]

2024 Jun 17;9(1):146. PMID: 38880808
J Extracell Vesicles

Exosomal Oleic Acid Promotes Lymphangiogenesis and Nodal Metastasis in Cervical Cancer via the AKT/mTOR Pathway. [Abstract]

2026 Jun;15(6):e70328. PMID: 42338019
Nat Commun

IGF1R-phosphorylated PYCR1 facilitates ELK4 transcriptional activity and sustains tumor growth under hypoxia. [Abstract]

2023 Sep 30;14(1):6117. PMID: 37777542
Phytomedicine

Paeoniflorin alleviates anxiety-like behaviors in sleep-deprived male mice by suppressing inflammation of the paraventricular nucleus of the hypothalamus. [Abstract]

2026 Jun:155:158111. PMID: 41931995
Cell Prolif

Dysregulation of Rho-Associated Coiled-Coil Protein Kinase1 Depletes Neural Stem Cell Pool and Impairs Hippocampal Neurogenesis After Traumatic Brain Injury. [Abstract]

2025 Aug 1:e70093. PMID: 40749978
Ecotoxicol Environ Saf

Hesperetin alleviates aflatoxin B1 induced liver toxicity in mice: Modulating lipid peroxidation and ferritin autophagy. [Abstract]

2024 Oct 1:284:116854. PMID: 39142113

Miransertib hydrochloride purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2024 Oct 1:284:116854. [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.
Drug Des Devel Ther

ED-71 Improves Bone Mass in Ovariectomized Rats by Inhibiting Osteoclastogenesis Through EphrinB2-EphB4-RANKL/OPG Axis. [Abstract]

2024 May 6:18:1515-1528. PMID: 38716369
Invest Ophthalmol Vis Sci

Hyperglycemia-Reduced Platelet-Derived Growth Factor-BB Expression Impairs Corneal Wound Healing in Diabetic Mice. [Abstract]

2025 Aug 1;66(11):61. PMID: 40856651

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.
Mol Pharm

Lipid Nanoparticle Delivery of iMDK Induces ATF3-Mediated Apoptosis in Sotorasib-Resistant KRAS Mutant Lung Cancer. [Abstract]

2025 Sep 1;22(9):5523-5532. PMID: 40758603

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.
Clin Pharmacol Ther

Mechanistic, functional and clinical aspects of pro-inflammatory cytokine mediated regulation of ADME gene expression in 3D human liver spheroids. [Abstract]

2023 Sep;114(3):673-685. PMID: 37307233
Biomedicines

TIRAP/Mal Positively Regulates TLR8-Mediated Signaling via IRF5 in Human Cells. [Abstract]

2022 Jun 22;10(7):1476. PMID: 35884781
FASEB J

Mechanical force modulates macrophage proliferation via Piezo1-AKT-Cyclin D1 axis. [Abstract]

2022 Aug;36(8):e22423. PMID: 35775626

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.
Virus Res

A conserved role for AKT in the replication of emerging flaviviruses in vertebrates and vectors. [Abstract]

2024 Oct:348:199447. PMID: 39117146
Hum Mol Genet

Mitofusin 2 mutation drives cell proliferation in Charcot-Marie-Tooth 2A fibroblasts. [Abstract]

2023 Jan 6;32(2):333-350. PMID: 35994048
Medicina (Kaunas)

The Synergistic Effect of Zuogui Pill and Eldecalcitol on Improving Bone Mass and Osteogenesis in Type 2 Diabetic Osteoporosis. [Abstract]

2023 Aug 3;59(8):1414. PMID: 37629706
J Chromatogr B Analyt Technol Biomed Life Sci

Development and validation of an LC-MS/MS assay for the quantification of Miransertib in human plasma and clinical application. [Abstract]

2026 May 29:1281:125161. PMID: 42224880
Biomed Pharmacother

2026 Sep:202:119803. PMID: 42537395
chemRxiv

2026 Jun 22.
bioRxiv

2025 May 06.
bioRxiv

2025 March 20.
University of North Carolina

2021.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (294 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

Bioz

Keywords

Miransertib hydrochloride

21 Cited Publications

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Miransertib hydrochloride

Publications Citing Use of MedChemExpress (MCE) Miransertib hydrochloride

Alle Akt Isoform-spezifische Produkte anzeigen

Alle Parasite Isoform-spezifische Produkte anzeigen