Referencia número: HY-19719

Miransertib

(Synonyms: ARQ-092)

19 Cited Publications

Revisión del cliente

Based on 19 publication(s) in Google Scholar

Miransertib (ARQ-092) 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 is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib is effective against Leishmania.

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Pureza: 99.32%
No. CAS: 1313881-70-7
Fòrmula: C₂₇H₂₄N₆
Peso molecular:432.52

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Miransertib Chemical Structure

No. CAS: 1313881-70-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (19)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Miransertib (ARQ-092) 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 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 is effective against Leishmania^[2].

IC₅₀ & Target^[1]^[2]

Akt1

2.7 nM (IC₅₀)

Leishmania

Akt3

8.1 nM (IC₅₀)

Akt2

14 nM (IC₅₀)

Akt1 E17K mutant

Ver todos los productos específicos de isoformas Akt :

Ver todos los productos específicos de isoformas Parasite :

Cellular Effect

Cell Line	Type	Value	Description	References
SW-620	GI₅₀	5.2 μM Compound: ARQ-092	Antiproliferative activity against human SW620 cells harboring KRAS mutant assessed as inhibition of cell growth incubated for 5 days by IncuCyte live-cell imaging analysis Antiproliferative activity against human SW620 cells harboring KRAS mutant assessed as inhibition of cell growth incubated for 5 days by IncuCyte live-cell imaging analysis	[PMID: 36197750]

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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1313881-70-7
Appearance Solid
Peso molecular 432.52
Fòrmula C₂₇H₂₄N₆
Color Off-white to yellow
SMILES

NC1=NC=CC=C1C2=NC3=CC=C(C4=CC=CC=C4)N=C3N2C5=CC=C(C6(N)CCC6)C=C5
Synonyms

ARQ-092
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (19)

All WBIn Vivo Imaging

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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 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 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 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 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 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
bioRxiv

2025 May 06.
bioRxiv

2025 March 20.
University of North Carolina

2021.

Solvente y solubilidad

In Vitro:

DMSO : 12.5 mg/mL (28.90 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

2.3120 mL

11.5602 mL

23.1203 mL

5 mM

0.4624 mL

2.3120 mL

4.6241 mL

10 mM

0.2312 mL

1.1560 mL

2.3120 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.25 mg/mL (2.89 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

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

Protocolo

Cell Assay^[1]

Anti-proliferative cellular assays are conducted using the CellTiter Non-Radioactive Cell Proliferation Assay, which utilizes the production of formazan from a tetrazolium compound by live cells. AN3CA and A2780 cells are obtained from the ATCC. AN3CA cells are cultured in DMEM, and A2780 cells are cultured in RPMI. Cells are plated in 96-well plates at 2,000-10,000 cells/well, cultured for 24 h, and treated with the test compound for 72 h at a final DMSO concentration no greater than 0.5% v/v. PMS stock reagent (0.92 mg/mL in DPBS) is diluted 20-fold in MTS stock reagent (2 mg/mL in DPBS), and this MTS/PMS mixture is diluted 5-fold into each well of the 96-well plate. The plates are incubated for 3-4 h, and the absorbance of formazan is measured at 490 nm. The data are normalized to the untreated controls, the dose-response curves are fit to a four-parameter logistic equation, and the IC₅₀ values are determined. All IC₅₀ values reported are the geometric mean of at least two independent determinations^[1].

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

Animal Administration^[2]

Mice^[2]
SHP2^Y279C/+ mice are used. Only male progeny are used for the experiments herein and all mice are maintained on outbred C57BL6/J backgrounds, backcrossed for more than 10 generations. Either vehicle or Miransertib (100 mg/kg body weight) is then daily administered by oral gavage for 4 weeks. Administration began at 12 weeks of age (after established hypertrophy is indicated), and continued for 4 weeks, until the mice reach 16 weeks of age. As controls, SHP2^+/+ and SHP2^Y279C/+ mice are treated with vehicle alone.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (297 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)
Instrucciones de manejo (2659 KB)

Referencias

[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

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3120 mL	11.5602 mL	23.1203 mL	57.8008 mL
	5 mM	0.4624 mL	2.3120 mL	4.6241 mL	11.5602 mL
	10 mM	0.2312 mL	1.1560 mL	2.3120 mL	5.7801 mL
	15 mM	0.1541 mL	0.7707 mL	1.5414 mL	3.8534 mL
	20 mM	0.1156 mL	0.5780 mL	1.1560 mL	2.8900 mL
	25 mM	0.0925 mL	0.4624 mL	0.9248 mL	2.3120 mL

Keywords

Miransertib

19 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Miransertib

Ver todos los productos específicos de isoformas Akt

Ver todos los productos específicos de isoformas Parasite

Actividad biológica

Chemical Information

Publications (19)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Miransertib Related Classifications

HY-19719 Related Classifications