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

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

目录号: HY-50706A 纯度: 99.48%
产品使用指南

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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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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    Description

    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].

    Molecular Weight

    555.76

    Formula

    C₁₇H₁₇BrClFN₄O₇S

    CAS No.

    943332-08-9

    SMILES

    OCCONC(C(C=C1C(N=CN1C)=C2F)=C2NC3=C(C=C(Br)C=C3)Cl)=O.O=S(O)(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

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