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AZD8055

Catalog No.S1555 1 Review(s)
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AZD8055 Chemical Structure

  • BEZ235 (NVP-BEZ235)

    BEZ235 (NVP-BEZ235)is a dual ATP-competitive phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM,respectively.

  • Deforolimus (Ridaforolimus)

    Deforolimus (Ridaforolimus) is a small-molecule inhibitor of mTOR.

  • PI-103

    PI-103 is a potent, cell-permeable, ATP-competitive PI3K family member inhibitor with IC50 of 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γ, respectively.

  • Rapamycin (Sirolimus)

    Rapamycin also known as Sirolimus & Rapamune is an mTOR inhibitor. Rapamycin Sirolimus inhibits cell motility by suppression of mTOR-mediated pathways.

  • Temsirolimus (Torisel)

    Temsirolimus (Torisel) is a mTOR inhibitor.

  • Everolimus (RAD001)

    Everolimus (RAD001) also known as SDZ-RAD, Certican, Zortress and Afinitorm is an mTOR inhibitor available at Selleck with IC50 of 0.63 nM.

  • Ku-0063794

    Ku-0063794 is an mTOR inhibitor, IC50 ~10 nM for mTORC1 and mTORC2, respectively.

  • WYE-354

    WYE-354 is an mTOR inhibitor with an IC50 of 5 nM.

  • GSK1059615

    GSK1059615 is a pan-PI3K reversible inhibitor,IC50:PI3Kα(0.4 nM), β (0.6 nM),γ (5 nM),δ (2 nM) and mTOR(12 nM).

  • XL765

    XL765 is a mixed mTOR/PI3k inhibitor with IC50 of 157, 39, 113, 9 and 43 nM for mTOR, p110α, β, γ and δ, respectively.

Biological Activity

AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. It inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphorylation of the mTORC2 substrate AKT and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 were fully inhibited by AZD8055, resulting in significant inhibition of cap-dependent translation. In vitro, AZD8055 potently inhibits proliferation and induces autophagy in H838 and A549 cells. In vivo, AZD8055 induces a dose-dependent pharmacodynamic effect on phosphorylated S6 and phosphorylated AKT at plasma concentrations leading to tumor growth inhibition. [1][2]

References on AZD8055
  • [1] Cancer Res 2010;70:288-298
  • [2] Autophagy May 16, 2010;6:4, 553-554
Molecular Weight (WM): 465.54
Formula:

C25H31N5O4

CAS No.: 1009298-09-2
Synonyms:
N/A
Dissolve in (25°C): DMSO ≥93mg/mL 
Water ≥2mg/mL 
Ethanol ≥15mg/mL 
Storage: 2 years-20°CPowder
1 week-4°Cin DMSO
1 month-80°in DMSO

Quality Control & MSDS

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COA H-NMR HPLC COA

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    After starved in serum-free medium for 24h , A549 cells incubated with the indicated concentrations of AZD8055 for 3h , followed by 20-minute stimolation of 100ng/ml EGF

     
     

     

  • After starved in serum-free medium for 24h , A549 cells incubated with the indicated concentrations of AZD8055 for 3h , followed by 20-minute stimolation of 100ng/ml EGF

     
     

     

  • Data independently produced by Dr. Zhang of Tianjin Medical University
    AZD8055 purchased from Selleck

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After starved in serum-free medium for 24h , A549 cells incubated with the indicated concentrations of AZD8055 for 3h , followed by 20-minute stimolation of 100ng/ml EGF

 
 

 

Data independently produced by Dr. Zhang of Tianjin Medical University

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