AZD8330

Catalog No.S2134 Synonyms: ARRY704

AZD8330 Chemical Structure

Molecular Weight(MW): 461.23

AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.

Size Price Stock Quantity  
In DMSO USD 310 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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4 Customer Reviews

  • iKras p53L/+ cells were treated with AZD8330 (50 nM), BKM120 (150 nM), or Rapamycin (20 nM) for 18 hr. As control, cells were cultured in the presence or absence of doxycycline for 24 hr, and cell lysates were blotted for phospho-Akt, phospho-Erk, phospho-S6, and Myc.

    Cell 2012 149(3), 656-70. AZD8330 purchased from Selleck.

    (B) MEK inhibition suppressed proliferation of lung cancer cells harboring mutant or wild-type EGFR. A549 and PC-9 cells were incubated in the presence of various concentrations of AZD-8330 or TAK-733. Cell extracts were prepared after 1 h of treatment and immunoblotted with the indicated antibodies (upper panel). Cell growth was measured by MTT assay after 72 h (lower panel).

    Oncotarget, 2016, 7(13):16273-81. AZD8330 purchased from Selleck.

  • Effect of MEK inhibitor AZD-8330 in A549 cells. A549 cells were incubated with increasing concentrations of AZD-8330 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.

    Dr.Wang from Southern Medical Hospital. AZD8330 purchased from Selleck.

    After starved in serum-free medium for 24 h, T47D cells incubated with the indicated concentrations of AZD8330 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.

    Dr. Zhang of Tianjin Medical University. AZD8330 purchased from Selleck.

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Biological Activity

Description AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
Targets
ERK phosphorylation [1] MEK1/2 [1]
0.4 nM 7 nM
In vitro

AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 200 other kinases including at concentrations up to 10 μM. AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines. [1]

In vivo In a Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model a single, 1.25 mg/kg oral dose of AZD8330 inhibits ERK phosphorylation by > 90% for between 4 and 8 hours. Doses as low as 0.4 mg/kg once daily are sufficient for > 80% tumor growth inhibition in the Calu-6 nude rat xenograft model. In the Calu-6 model, AZD8330 inhibits tumor growth in a dose-dependent fashion, at 0.3 mg/kg and 1.0 mg/kg once daily. [1]

Protocol

Kinase Assay:

[2]

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MEK1 enzymatic assays:

NH2-terminal hexahistidine tagged, constitutively active MEK1 (S218D, S222D ΔR4F) is expressed in baculovirus-infected Hi5 insect cells and purified by immobilized metal affinity chromatography, ion exchange, and gel filtration. The activity of MEK1 is assessed by measuring the incorporation of [γ- 33P]phosphate from [γ-33P]ATP onto ERK2. The assay is carried out in a 96-well polypropylene plate with an incubation mixture (100 μL) composed of 25 mM HEPES (pH 7.4), 10 mM MgCl2, 5 mM β-glycerolphosphate, 100 μM sodium orthovanadate, 5 mM DTT, 5 nM MEK1, 1 μM ERK2, and 0 to 80 nM AZD8330 (final concentration of 1% DMSO). The reactions are initiated by the addition of 10 μM ATP (with 0.5 μC k[γ-33P]ATP/well) and incubated at room temperature for 45 min. An equal volume of 25% trichloracetic acid is added to stop the reaction and precipitate the proteins. Precipitated proteins are trapped onto glass fiber B filter plates, excess labeled ATP is washed off with 0.5% phosphoric acid, and radioactivity is counted in a liquid scintillation counter. ATP dependence is determined by varying the amount of ATP in the reaction mixture. The data are globally fitted.
Cell Research:

[1]

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  • Cell lines: Malme-3M melanoma cells
  • Concentrations: ~10 μM
  • Incubation Time: 1 hour
  • Method:

    Malme-3M melanoma cells are plated in 96-wells and treated with various concentrations of AZD8330 for 1 hour at 37 °C. The cells are fixed, permeabilized, and incubated with an anti-phospho-ERK antibody and an anti-ERK 1/2 antibody. Plates are washed and fluorescently-labeled secondary antibodies are added. Plates are analyzed on a LICOR fluorescence imager. The pERK signal is normalized to the total ERK signa


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female nude rats (NIH rnu/rnu) with Calu-6 cells, nude rats with SW620 cells
  • Formulation: 0.5% HPMC-0.1% Tween
  • Dosages: 0.3 mg/kg, 1 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (199.46 mM)
Ethanol 92 mg/mL (199.46 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% hydroxyethyl cellulose+0.1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* 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 461.23
Formula

C16H17FIN3O4

CAS No. 869357-68-6
Storage powder
in solvent
Synonyms ARRY704

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00454090 Completed Cancer AstraZeneca March 2007 Phase 1

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID