1. MAPK/ERK Pathway
  2. MEK

Selumetinib (Synonyms: AZD6244; ARRY-142886)

Cat. No.: HY-50706 Purity: 99.39%
Handling Instructions

Selumetinib is a highly potent MEK inhibitor, with an IC50 value of 14 nM against MEK1.

For research use only. We do not sell to patients.
Selumetinib Chemical Structure

Selumetinib Chemical Structure

CAS No. : 606143-52-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
50 mg USD 72 In-stock
100 mg USD 96 In-stock
200 mg USD 156 In-stock
500 mg USD 300 In-stock
1 g USD 468 In-stock
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Customer Review

    Selumetinib purchased from MCE. Usage Cited in: Clin Cancer Res. 2014 Nov 1;20(21):5483-95.

    Effects of GSK1904529A and AZD6244 as single agents, respectively, on mediators of IGF-1R- and ERK1/ERK2-signaling pathways.(A–B) Effect of GSK1904529A on phosphorylation of IGF-1R (A) and Erk1/Erk2 (B). (C–E) Effect of AZD6244 on phosphorylation of IGF-1R (C), IGF-1R protein expression levels (D), and phosphorylation of Erk1/Erk2 (E). GSK1904529A is observed to inhibit phosphorylation of IGF-1R in a concentration-dependent manner (A), however shows no inhibitory activity against phosphorylation

    Selumetinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14835-14846.

    MEK inhibition results in reduced ERK phosphorylation.A. Western blot analysis of SEM and KOPN8 exposed to 500 nM of MEK inhibitor or vehicle control (DMSO) for 6, 24 and 48 hours. Both cell lines almost completely lose ERK phosphorylation (p-ERK), while total ERK (t-ERK) levels remain unaffected. B. Analysis of MEK phosphorylation (p-MEK) suggests exposure to MEK162 and Selumetinib results in enhanced MEK phosphorylation in both cell lines, whereas total MEK (t-MEK) levels remain constant.

    Selumetinib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Feb;16(2):334-343.

    Selumetinib treatment results in decreased phosphorylation of ERK1/2. Effect of Selumetinib on the expression and phosphorylation of ERK and AKT in the gastrocnemius muscle of cancer cachexia model.

    Selumetinib purchased from MCE. Usage Cited in: Genome Med. 2016 Oct 31;8(1):116.

    Phosphorylation level of RPS6 upon Temsirolimus treatment. The effective target engagement is confirmed in Temsirolimus-treated tumors by showing reduced phosphorylation of downstream mTOR targets, RPS6 and 4EBP1, and an associated increase in autophagy (LC3A/B).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    Selumetinib is a highly potent MEK inhibitor, with an IC50 value of 14 nM against MEK1.

    IC50 & Target

    IC50: 14 nM (MEK1)

    In Vitro

    Selumetinib causes a time- and dose-dependent reduction in DNA synthesis and cell viability in primary, induces growth arrest and apoptosis associated with the inactivation of ERK in primary 2-1318 cells[1]. Selumetinib (1µM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells[2]. Selumetinib (ARRY-142886) results in the growth inhibition of several cell lines containing B-Raf and Ras mutations but has no effect on a normal fibroblast cell line[3].

    In Vivo

    Selumetinib (AZD6244, 50 and 100 mg/kg, p.o.) decreases the growth rate of 4-1318 xenografts in a dose-dependent manner; AZD6244 when given at the dose of 50 mg/kg also significantly suppresses the growth of the 5-1318, 2-1318, 26-1004, and 29-1104 xenografts[1]. Selumetinib (ARRY-142886, 10, 25, 50, or 100 mg/kg, p.o.) is capable of inhibiting both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice. Tumor regressions are also seen in a BxPC3 xenograft model[3].

    Clinical Trial
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.1849 mL 10.9247 mL 21.8493 mL
    5 mM 0.4370 mL 2.1849 mL 4.3699 mL
    10 mM 0.2185 mL 1.0925 mL 2.1849 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay

    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 selumetinib (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay

    Selumetinib is dissolved in DMSO to a final concentration of 20 mM. 

    Primary HCC cells are plated at a density of 2.0×104 per well in growth medium. After 48 h in growth medium, the cell monolayer is rinsed twice with MEM. Cells are treated with various concentrations of Selumetinib (AZD6244, 0, 0.5, 1.0, 2.0, 3.0, and 4.0 μM) for 24 or 48 h. Cell viability is determined by the MTT assay. Cell proliferation is assayed using a bromodeoxyuridine kit as described by the manufacturer. Experiments are repeated at least thrice, and the data are expressed as mean±SE. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration

    Selumetinib is suspended in water at an appropriate concentration.

    To investigate the effects of Selumetinib (AZD6244) on HCC xenografts, AZD6244 is suspended in water at an appropriate concentration. Mice bearing HCC xenografts are p.o. given, twice a day, with either 100 μL of water (n=12) or 50 mg (n=12) or 100 mg (n=12) of AZD6244 per kilogram of body weight for 21 days, starting from day 7 after tumor implantation. Growth of established tumor xenografts is monitored at least twice weekly by Vernier caliper measurement of the length (a) and width (b) of the tumor. Tumor volume is calculated as (a × b2)/2. Animals are sacrificed 3 h after the last dose of ADZ6244, and body and tumor weights are recorded, with the tumors harvested for analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight




    CAS No.




    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 34 mg/mL

    Selumetinib is resuspended in N-Methyl-2-pyrrolidone (NMP) to create a stock solution and diluted in PTD buffer (30 % PEG-400; 5 % Tween 80; 65 % Dextrose water, D5W) before drug dosing[4].
    Selumetinib (AZD6244) is reconstituted in 0.5% methylcellulose and 0.4% polysorbate (Tween80)[5].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.


    Purity: 99.39%

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