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

Selumetinib sulfate (Synonyms: AZD6244 sulfate; ARRY-142886 sulfate)

目录号: HY-50706A 纯度: 99.48%

Selumetinib (AZD6244) 是一种高效选择性的,非 ATP 竞争性的 MEK1/2 抑制剂, 抑制 MEK1 的 IC50 为 14 nM。Selumetinib (AZD6244) 抑制 MEK1/2 磷酸化水平。

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Selumetinib sulfate Chemical Structure

Selumetinib sulfate Chemical Structure

CAS No. : 943332-08-9

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1  mL in DMSO ¥660 In-stock
50 mg ¥600 In-stock
100 mg ¥958 In-stock
200 mg ¥1300 In-stock
500 mg ¥2600 In-stock
1 g ¥4500 In-stock
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Customer Review

Other Forms of Selumetinib sulfate:

Top Publications Citing Use of Products

    Selumetinib sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献


    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.

    In Vitro

    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].

    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
    Molecular Weight




    CAS No.





    Room temperature in continental US; may vary elsewhere.

    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (89.97 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7993 mL 8.9967 mL 17.9934 mL
    5 mM 0.3599 mL 1.7993 mL 3.5987 mL
    10 mM 0.1799 mL 0.8997 mL 1.7993 mL

    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.50 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.50 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.50 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
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    SelumetinibAZD6244ARRY-142886AZD 6244AZD-6244ARRY142886ARRY 142886MEKApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit


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