Miransertib (ARQ 092) HCl

Catalog No.S8339 Synonyms: Miransertib

Miransertib (ARQ 092) HCl Chemical Structure

Molecular Weight(MW): 468.98

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

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Biological Activity

Description ARQ 092 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

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].

In vivo Short-term oral administration of ARQ 092 or hydroxyurea, a main therapy for sickle cell disease, diminishes heterotypic cell-cell interactions in venules of sickle cell disease mice challenged with TNF-α. 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].

Protocol

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Male SCD mice
  • Formulation: Phosphoric acid (0.01 M)
  • Dosages: 100 mg/10ml/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (159.92 mM)
Ethanol 4 mg/mL (8.52 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 468.98
Formula

C27H25ClN6

CAS No. 1313883-00-9
Storage powder
Synonyms Miransertib

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID