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Chemical Structure| 1313881-70-7 Chemical Structure| 1313881-70-7

Structure of Miransertib
CAS No.: 1313881-70-7

Chemical Structure| 1313881-70-7

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ARQ-092 is an orally bioavailable, selective, and potent allosteric Akt inhibitor with IC50 of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.

Synonyms: ARQ-092

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Product Details of Miransertib

CAS No. :1313881-70-7
Formula : C27H24N6
M.W : 432.52
SMILES Code : NC1=NC=CC=C1C2=NC3=CC=C(C4=CC=CC=C4)N=C3N2C5=CC=C(C6(N)CCC6)C=C5
Synonyms :
ARQ-092
MDL No. :MFCD30187510

Safety of Miransertib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H373
Precautionary Statements:P260-P314-P501

Related Pathways of Miransertib

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • Akt3

    Akt3, IC50:16 nM

  • Akt1

    Akt1, IC50:5 nM

  • Akt2

    Akt2, IC50:4.5 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
BC-3 1.5 µM 24 h Both miransertib and MK-4440 reduced the number of live BC-3 cells and decreased the phosphorylation levels of Akt, but had a minimal effect on the phosphorylation of downstream targets. PMC8253055
BJAB 1.06 µM 72 h Both miransertib and MK-4440 reduced the number of live BJAB cells and decreased the phosphorylation levels of Akt, but had a minimal effect on the phosphorylation of downstream targets. PMC8253055
FL-18 1 µM and 5 µM 72 h Both miransertib and MK-4440 reduced the number of live FL-18 cells and decreased the phosphorylation levels of Akt and its downstream targets such as FOXO1, S6K, and S6. PMC8253055
Pik3caH1047R ECs 2 µM 24 h To assess the impact of miransertib on the PI3K/AKT signaling pathway, results showed that miransertib significantly reduced p-Akt and p-Pras40 levels and regulated the expression of Ang2 and cell cycle regulators. PMC9260211
HUVEC-vPK cells 1 µM 24 h Inhibition of AKT phosphorylation, leading to Caspase-3 cleavage and induction of apoptosis PMC10585003
Caov3 1 μmol/l 2 hours Evaluate the combined effect of ARQ 092 and ARQ 087, results showed only inhibition of pS6 PMC5404396
IGROV-1 1 μmol/l 72 hours Evaluate the combined effect of ARQ 092 and ARQ 087, results showed no changes in cell cycle and apoptosis PMC5404396
AN3CA 1 μmol/l 72 hours Evaluate the combined effect of ARQ 092 and ARQ 087, results showed G1 phase cell cycle arrest and increased apoptosis PMC5404396

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice FL-18 xenograft model Oral 100 mg/kg Once daily for three weeks Miransertib alone or in combination with sirolimus significantly reduced tumor growth in the FL-18 xenograft model. PMC8253055
Mice PIK3CA-related capillary venous malformation mouse model Oral 30 mg/kg Once daily, continuous treatment Miransertib showed some efficacy in treating PIK3CA-related capillary venous malformation in mice, slightly reducing venous malformation volumes and extending lifespan, but it did not significantly impact platelet levels, anemia, or histological abnormalities. PMC11180659
Mice Pik3caH1047R mutant mouse model Intraperitoneal injection 75 mg/kg and 35 mg/kg Administered at P1 and P2 days, continued until P6 days To evaluate the preventive and therapeutic effects of miransertib on PI3K-driven vascular malformations, results showed that miransertib effectively prevented and induced the regression of vascular malformations and inhibited the PI3K signaling pathway. PMC9260211
C57BL/6 mice Myocardial ischemia-reperfusion injury model Intraperitoneal injection 120 mg/kg Single dose 1 hour before surgery To investigate the protective effect of Miransertib on myocardial ischemia-reperfusion injury, results showed that Miransertib reversed the alleviating autophagy effect of Metformin by inhibiting the Akt signaling pathway PMC7415420

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03094832 PIK3CA-Related Overgrowth Spec... More >>trum (PROS)/Proteus Syndrome Less << PHASE1|PHASE2 TERMINATED 2022-04-11 Children's Hospital of Atlanta... More >> ( Site 0107), Atlanta, Georgia, 30342, United States|Ann & Robert H. Lurie Children's Hospital of Chicago ( Site 0101), Chicago, Illinois, 60611, United States|Boston Children's Hospital ( Site 0089), Boston, Massachusetts, 02115, United States|Cincinnati Children's Hospital Medical Center ( Site 0102), Cincinnati, Ohio, 45229, United States|Texas Children's Hospital ( Site 0104), Houston, Texas, 77030, United States|Seattle Childrens Hospital ( Site 0103), Seattle, Washington, 98105, United States|Hunter Genetics ( Site 0201), Waratah NSW, New South Wales, 2298, Australia|Ospedale Pediatrico Bambino Gesu ( Site 0087), Rome, Roma, 00165, Italy|Universita di Catania ( Site 0088), Catania, 95123, Italy|Fondazione Policlinico Universitario A. Gemelli ( Site 0052), Roma, 00168, Italy|Hospital Sant Joan ( Site 0601), Esplugues de Llobregat, Barcelona, 08950, Spain Less <<
NCT04980872 PIK3CA-Related Overgrowth Spec... More >>trum (PROS)/Proteus Syndrome (PS) Less << PHASE2 ACTIVE_NOT_RECRUITING 2030-02-07 Children's Healthcare of Atlan... More >>ta - Egleston Hospital ( Site 0107), Atlanta, Georgia, 30322, United States|Boston Children's Hospital ( Site 0089), Boston, Massachusetts, 02115, United States|Cincinnati Children's Hospital Medical Center-Hematology ( Site 0102), Cincinnati, Ohio, 45229, United States|Texas Children's Hospital ( Site 0104), Houston, Texas, 77030, United States|Seattle Children's Hospital ( Site 0103), Seattle, Washington, 98105, United States|John Hunter Hospital ( Site 0203), Newcastle, New South Wales, 2305, Australia|Bundaberg Base Hospital ( Site 0202), Bundaberg, Queensland, 4670, Australia|Hospital Araújo Jorge ( Site 0801), Goiania, Goias, 74605070, Brazil|Fondazione Policlinico Universitario Agostino Gemelli ( Site 0052), Roma, Lazio, 00168, Italy|Ospedale Pediatrico Bambino Gesù-Centro Trials ( Site 0087), Rome, Roma, 00165, Italy|Great Ormond Street Hospital ( Site 0701), London, London, City Of, WC1N 3JH, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL

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