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  • 维罗非尼

    Vemurafenib (PLX4032)

    维罗非尼
    产品编号 CFN60058
    CAS编号 918504-65-1
    分子式 = 分子量 C23H18ClF2N3O3S = 489.92
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Alkaloids
    植物来源
    ChemFaces的产品在影响因子大于5的优秀和顶级科学期刊中被引用
    提供自定义包装
    产品名称 产品编号 CAS编号 包装 QQ客服
    维罗非尼 CFN60058 918504-65-1 1mg QQ客服:1457312923
    维罗非尼 CFN60058 918504-65-1 5mg QQ客服:1457312923
    维罗非尼 CFN60058 918504-65-1 10mg QQ客服:1457312923
    维罗非尼 CFN60058 918504-65-1 20mg QQ客服:1457312923
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    ChemFaces的产品在许多优秀和顶级科学期刊中被引用

    Cell. 2018 Jan 11;172(1-2):249-261.e12.
    doi: 10.1016/j.cell.2017.12.019.
    IF=36.216(2019)

    PMID: 29328914

    Cell Metab. 2020 Mar 3;31(3):534-548.e5.
    doi: 10.1016/j.cmet.2020.01.002.
    IF=22.415(2019)

    PMID: 32004475

    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
    doi: 10.1016/j.molcel.2017.10.022.
    IF=14.548(2019)

    PMID: 29149595

    ACS Nano. 2018 Apr 24;12(4): 3385-3396.
    doi: 10.1021/acsnano.7b08969.
    IF=13.903(2019)

    PMID: 29553709

    Nature Plants. 2016 Dec 22;3: 16206.
    doi: 10.1038/nplants.2016.205.
    IF=13.297(2019)

    PMID: 28005066

    Sci Adv. 2018 Oct 24;4(10): eaat6994.
    doi: 10.1126/sciadv.aat6994.
    IF=12.804(2019)

    PMID: 30417089
    我们的产品现已经出口到下面的研究机构与大学,并且还在增涨
  • University of Wuerzburg (Germany)
  • Universiti Malaysia Pahang (Malaysia)
  • Pennsylvania State University (USA)
  • University of Toulouse (France)
  • Utrecht University (Netherlands)
  • Universidad de Antioquia (Colombia)
  • Universidade Federal de Pernambuco (UFPE) (Brazil)
  • Institute of Chinese Materia Medica (China)
  • Colorado State University (USA)
  • Institute of Pathophysiology Medical University of Vienna (Austria)
  • University of Maryland (USA)
  • Aarhus University (Denmark)
  • Texas A&M University (USA)
  • Institute of Bioorganic Chemistry Polish Academy of Sciences (Poland)
  • More...
  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Pharmaceutics.2021, 13(7):1028.
  • Anal Bioanal Chem.2016, 408(1):177-90.
  • Phytomedicine.2017, 24:77-86
  • J.Pharm. & Biome. Anal.2023, 2: 100018.
  • LWT2020, 126:109313
  • Drug Chem Toxicol.2020, 1-14.
  • Phytother Res.2018, 32(5):923-932
  • Plant Sci.2020, 301:110656.
  • Academic J of Second Military Medical University2018, 39(11)
  • Molecules.2017, 22(12)
  • BMB Rep.2020, 53(4):218-222.
  • Histol Histopathol.2022, 18518.
  • Planta Med.2019, 85(3):217-224
  • Viruses.2021, 13(11):2118.
  • J Anal Toxicol.2021, bkab015.
  • J Nat Prod.2023, 86(2):264-275.
  • Anal Bioanal Chem.2023, 415(9):1641-1655.
  • J Holistic Integrative Pharm.2023, 4(1):14-28
  • Acta Chromatographica2016, 29(3)
  • Pharmacol Res.2020, 161:105205.
  • Int J Mol Sci.2018, 19(9):E2681
  • Sci Rep.2017, 7:467-479
  • Neurotoxicology.2022, 91:218-227.
  • ...
  • 生物活性
    Description: Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.
    Targets: B-RafV600E | Autophagy
    In vitro:
    Nature,2012 Jan 26;483(7387):100-3.
    Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR.[Pubmed: 22281684]
    Inhibition of the BRAF(V600E) oncoprotein by the small-molecule drug PLX4032 (vemurafenib) is highly effective in the treatment of melanoma. However, colon cancer patients harbouring the same BRAF(V600E) oncogenic lesion have poor prognosis and show only a very limited response to this drug.
    METHODS AND RESULTS:
    To investigate the cause of the limited therapeutic effect of PLX4032 in BRAF(V600E) mutant colon tumours, here we performed an RNA-interference-based genetic screen in human cells to search for kinases whose knockdown synergizes with BRAF(V600E) inhibition. We report that blockade of the epidermal growth factor receptor (EGFR) shows strong synergy with BRAF(V600E) inhibition. We find in multiple BRAF(V600E) mutant colon cancers that inhibition of EGFR by the antibody drug cetuximab or the small-molecule drugs gefitinib or erlotinib is strongly synergistic with BRAF(V600E) inhibition, both in vitro and in vivo. Mechanistically, we find that BRAF(V600E) inhibition causes a rapid feedback activation of EGFR, which supports continued proliferation in the presence of BRAF(V600E) inhibition. Melanoma cells express low levels of EGFR and are therefore not subject to this feedback activation. Consistent with this, we find that ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032.
    CONCLUSIONS:
    Our data suggest that BRAF(V600E) mutant colon cancers (approximately 8-10% of all colon cancers), for which there are currently no targeted treatment options available, might benefit from combination therapy consisting of BRAF and EGFR inhibitors.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.0411 mL 10.2057 mL 20.4115 mL 40.823 mL 51.0287 mL
    5 mM 0.4082 mL 2.0411 mL 4.0823 mL 8.1646 mL 10.2057 mL
    10 mM 0.2041 mL 1.0206 mL 2.0411 mL 4.0823 mL 5.1029 mL
    50 mM 0.0408 mL 0.2041 mL 0.4082 mL 0.8165 mL 1.0206 mL
    100 mM 0.0204 mL 0.1021 mL 0.2041 mL 0.4082 mL 0.5103 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    部分图片展示
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    3-氧代坡模酸甲酯; 3-Oxopomolic acid methyl ester CFN92820 14440-23-4 C31H48O4 = 484.7 5mg QQ客服:1413575084
    苦参醇B; Kushenol B CFN92348 99217-64-8 C30H36O6 = 492.6 5mg QQ客服:2159513211
    巨大戟醇-3-当归酸酯; Ingenol 3-Angelate CFN90924 75567-37-2 C25H34O6 = 430.5 5mg QQ客服:3257982914
    Borapetoside B; Borapetoside B CFN96298 104901-05-5 C27H36O12 = 552.6 5mg QQ客服:3257982914

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