1. MAPK/ERK Pathway
    Apoptosis
  2. MEK
    Apoptosis
  3. Selumetinib

Selumetinib (Synonyms: AZD6244; ARRY-142886)

製品番号: HY-50706 純度: 99.87%
取扱説明書

Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

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Selumetinib 構造式

Selumetinib 構造式

CAS 番号 : 606143-52-6

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
50 mg USD 72 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 96 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 156 在庫あり
Estimated Time of Arrival: December 31
500 mg USD 300 在庫あり
Estimated Time of Arrival: December 31
1 g USD 468 在庫あり
Estimated Time of Arrival: December 31
5 g   お問い合わせ  
10 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 39 publication(s) in Google Scholar

Other Forms of Selumetinib:

Top Publications Citing Use of Products

    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: Clin Cancer Res. 2014 Nov 1;20(21):5483-95.

    Effects of AZD6244 as single agents, respectively, on mediators of IGF-1R- and ERK1/ERK2-signaling pathways.Effect of AZD6244 on IGF-1R protein expression levels, and phosphorylation of Erk1/Erk2.

    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: Drug Des Devel Ther. 2018 Apr 19;12:911-920.

    Immunoblotting demonstrates that AZD6244 can effectively restore upregulation of LC3-II/I and downregulation of p62 induced by RAD001 in 786-O and A498 cells.

    Selumetinib purchased from MCE. Usage Cited in: PLoS One. 2018 Jul 5;13(7):e0200014.

    Representative immunoblots of control and NHARAS treated with Selumetinib for 24 h.

    Selumetinib purchased from MCE. Usage Cited in: Sci Signal. 2018 Oct 30;11(554). pii: eaar6795. 

    MEK1 mutants with in-frame deletions of the β3-αC loop exhibit differential resistance to MEK inhibitors (GSK1120212, GDC0623, cobimetinib, AZD6244, and binimentinib).

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    製品説明

    Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

    IC50 & Target[3][4]

    MEK

    12 nM (IC50)

    MEK1

    14 nM (IC50)

    MEK2

     

    体外実験

    Selumetinib (AZD6244) 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 (AZD6244) (1µM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells[2].
    Selumetinib (AZD6244) 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].

    体内実験

    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].

    臨床実験
    分子量

    457.68

    分子式

    C₁₇H₁₅BrClFN₄O₃

    CAS 番号

    606143-52-6

    SMILES

    O=C(C1=C(C(F)=C2N=CN(C2=C1)C)NC3=CC=C(C=C3Cl)Br)NOCCO

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 20.83 mg/mL (45.51 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    キナーゼ実験
    [3]

    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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    細胞実験
    [1]

    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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [1]

    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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 99.87%

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    Keywords:

    SelumetinibAZD6244ARRY-142886AZD 6244AZD-6244ARRY142886ARRY 142886MEKApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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    製品名:
    Selumetinib
    製品番号:
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