Home PI3K/Akt/mTOR Akt inhibitor Miransertib (ARQ 092) HCl For research use only.

Miransertib (ARQ 092) HCl

Synonyms: Miransertib

Miransertib (ARQ 092) HCl is a novel, orally bioavailable and selective AKT pathway inhibitor exhibiting a manageable safety profile among patients with advanced solid tumors.

Miransertib (ARQ 092) HCl Chemical Structure

Miransertib (ARQ 092) HCl Chemical Structure

CAS No. 1313883-00-9

Purity & Quality Control

Miransertib (ARQ 092) HCl Related Products

Signaling Pathway

Akt Signaling Pathways

Akt Signaling Pathway

Biological Activity

Description Miransertib (ARQ 092) HCl is a novel, orally bioavailable and selective AKT pathway inhibitor exhibiting a manageable safety profile among patients with advanced solid tumors.
Targets
Akt2 [1]
(Cell-free assay)		 Akt1 [1]
(Cell-free assay)		 Akt3 [1]
(Cell-free assay)
4.5 nM 5 nM 16 nM
In vitro
In vitro

ARQ 092 blocks membrane translocation of inactive AKT and even dephosphorylates the membrane-associated active form, thereby perturbing AKT activity. Treatment with 50-500 nM ARQ 092 significantly blocks αMβ2 integrin function in neutrophils and reduces P-selectin exposure and glycoprotein Ib/IX/V-mediated agglutination in platelets[2]. In a large panel of diverse cancer cell lines, ARQ 092 inhibits proliferation across multiple tumor types but are most potent in leukemia, breast, endometrial, and colorectal cancer cell lines. Moreover, inhibition by ARQ 092 is more prevalent in cancer cell lines containing PIK3CA/PIK3R1 mutations compared to those with wt-PIK3CA/PIK3R1 or PTEN mutations[1]. ARQ 092 targets the PI3K/AKT pathway and AKT specifically and reduces phosphorylation of GSK3α and GSK3β in mutation-positive cells[3].
Cell Research Cell lines MDA-MB-453 cells; NCI-H1650 cells; KU-19-19 cells
Concentrations 0, 0.012, 0.037, 0.11, 0.33, and 1 μM
Incubation Time 2 h
Method

Cells (MDA-MB-453: 1.5×106; NCI-H1650: 1×106; KU-19-19: 0.7×106) are plated into 6 well plates, left overnight, and then treated with full media containing different concentrations (0, 0.012, 0.037, 0.11, 0.33, and 1 μM) of AKT inhibitors (ARQ 092, ARQ 751, MK-2206, GDC-0068) for 2 hours. Cells are treated under designated conditions and lysates are extracted. Proteins are resolved from extracts using SDS-PAGE followed by immunoblotting.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT / p-PRAS40 / PRAS40 / p-ERK / ERK / p-FOXO1 / p-GSKβ(S9) / pAS160(S318) / pBAD / pS6 / p-4EBP1 26469692
Growth inhibition assay Cell viability 30399177
In Vivo
In vivo

ARQ 092 is well tolerated at a continuous daily dose of 60 mg or a dose of 600 mg when administered once a week, for several months. ARQ 092 is likely to inhibit the activity of all AKT isoforms in intravascular cells and thereby attenuates the process of thrombosis and inflammation in SCD patients[2]. ARQ 092 is highly active in a subset of endometrial tumors that harbor PI3K pathway gene mutations[1].
Animal Research Animal Models Male SCD mice
Dosages 100 mg/10ml/kg
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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)
 November 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 468.98 Formula

C27H25ClN6
CAS No. 1313883-00-9 SDF Download Miransertib (ARQ 092) HCl SDF
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.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (159.92 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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