Home > Signaling Pathways>PI3K/Akt/mTOR>Akt>Miransertib HCl (ARQ 092; MK-7075)
Miransertib HCl (ARQ 092; MK-7075)

This product is for research use only, not for human use. We do not sell to patients.

Miransertib HCl (ARQ 092; MK-7075)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$750Check With Us
500mg$1350Check With Us
1g$2025Check With Us

Cat #: V3318 CAS #: 1313883-00-9 Purity ≥ 98%

Description: Miransertib HCl (formerly known as ARQ-092; MK7075), the HCl salt of Miransertib, is a novel, orally bioactive and selective allosteric inhibitor of AKT anticancer activity.

References: 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.

Top Publications Citing Invivochem Products
Publications Citing InvivoChem Products

Product Promise

Promise
Molecular Weight (MW)468.99
Molecular FormulaC27H25ClN6
CAS No.1313883-00-9
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: >50 mg/mLr
Water: N/Ar
Ethanol: N/A
SMILES CodeNC1=NC=CC=C1C2=NC3=CC=C(C4=CC=CC=C4)N=C3N2C5=CC=C(C6(N)CCC6)C=C5.[H]Cl
SynonymsARQ092 hydrochloride; MK-7075; ARQ-092 hydrochloride; MK7075; ARQ 092; 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine hydrochloride
ProtocolIn VitroIn 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).
In VivoMiransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinom. 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.1322 mL10.6612 mL21.3224 mL42.6448 mL
5mM0.4264 mL2.1322 mL4.2645 mL8.5290 mL
10mM0.2132 mL1.0661 mL2.1322 mL4.2645 mL
20mM0.1066 mL0.5331 mL1.0661 mL2.1322 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.