1. PI3K/Akt/mTOR Anti-infection
  2. Akt Parasite
  3. Miransertib hydrochloride

Miransertib hydrochloride  (Synonyms: ARQ-092 hydrochloride)

Cat. No.: HY-19719A Purity: 99.74%
Data Sheet SDS COA Handling Instructions

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.

Miransertib hydrochloride Chemical Structure

Miransertib hydrochloride Chemical Structure

CAS No. : 1313883-00-9

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Miransertib hydrochloride:

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  • Biological Activity

  • Purity & Documentation

  • References

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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
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 t1/2 values of 17 h in rats versus 7 h in monkeys. The Cmax is 198 ng/mL and 258 ng/mL and the AUCinf 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.

Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT03094832ArQule, Inc. (a wholly owned subsidiary of Merck Sharp and Dohme, a subsidiary of Merck & Co., Inc.)|Worldwide Clinical Trials
PIK3CA-Related Overgrowth Spectrum (PROS)+Proteus Syndrome
May 16, 2017Phase 1|Phase 2
NCT01473095ArQule, Inc. (a wholly owned subsidiary of Merck Sharp and Dohme, a subsidiary of Merck & Co., Inc.)
Solid Tumor|Malignant Lymphoma|Tumor
November 2011Phase 1
NCT03317366ArQule, Inc. (a wholly owned subsidiary of Merck Sharp and Dohme, a subsidiary of Merck & Co., Inc.)
Proteus Syndrome|PIK3CA-Related Overgrowth Spectrum (PROS)|Growth Disorders
Molecular Weight

468.98

Formula

C27H25ClN6

CAS No.
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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
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. 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.74%

References

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

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
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  • Do most proteins show cross-species activity?

    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
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