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Miransertib (ARQ-092) Akt inhibitor

Name: Miransertib (ARQ-092)
Brand: Selleck Chemicals
SKU: S6811
Availability: InStock
Rating: 5 (10 reviews)

Cat.No.S6811

Miransertib (ARQ-092) is a potent, selective and orally bioavailable allosteric inhibitor of Akt with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.

Miransertib (ARQ-092) Akt inhibitor Chemical Structure

Quality Control

Batch: S681101 DMSO]8 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.45%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS/MSDS
Datasheet

99.45

Related Targets	PI3K mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PI4K PP2A
Other Akt Inhibitors	SC79 AZD5363 (Capivasertib) MK-2206 Dihydrochloride Ipatasertib (GDC-0068) Perifosine GSK690693 Triciribine (API-2) Afuresertib (GSK2110183) CCT128930 A-674563 HCl

Solubility

In vitro
Batch:

DMSO : 8 mg/mL (18.49 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.4mg/ml (0.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	432.52	Formula	C₂₇H₂₄N₆	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1313881-70-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			SMILES	C1CC(C1)(C2=CC=C(C=C2)N3C4=C(C=CC(=N4)C5=CC=CC=C5)N=C3C6=C(N=CC=C6)N)N

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	Akt1 (Cell-free assay) 2.7 nM Akt3 (Cell-free assay) 8.1 nM Akt2 (Cell-free assay) 14 nM
References	[1] https://pubmed.ncbi.nlm.nih.gov/27305487/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-02-07)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04980872	ACTIVE_NOT_RECRUITING	PIK3CA-Related Overgrowth Spectrum (PROS)/Proteus Syndrome (PS)	Merck Sharp & Dohme LLC	2021-11-02	PHASE2
NCT04316546	ACTIVE_NOT_RECRUITING	Proteus Syndrome	National Human Genome Research Institute (NHGRI)	2022-05-20	PHASE2
NCT03094832	TERMINATED	PIK3CA-Related Overgrowth Spectrum (PROS)/Proteus Syndrome	ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA)	2017-05-16	PHASE1; PHASE2
NCT02476955	TERMINATED	Solid Tumors; Ovarian Cancer; Endometrial Cancer	ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA)	2015-06-09	PHASE1
NCT02594215	COMPLETED	Proteus Syndrome	National Human Genome Research Institute (NHGRI)	2015-11-16	PHASE1
NCT01473095	COMPLETED	Solid Tumor; Malignant Lymphoma; Tumor	ArQule, Inc., a subsidiary of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc. (Rahway, NJ USA)	2011-11	PHASE1

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