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  • 塞卡替尼

    Saracatinib (AZD0530)

    塞卡替尼
    产品编号 CFN60031
    CAS编号 379231-04-6
    分子式 = 分子量 C27H32ClN5O5 = 542.03
    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
    塞卡替尼 CFN60031 379231-04-6 1mg QQ客服:1413575084
    塞卡替尼 CFN60031 379231-04-6 5mg QQ客服:1413575084
    塞卡替尼 CFN60031 379231-04-6 10mg QQ客服:1413575084
    塞卡替尼 CFN60031 379231-04-6 20mg QQ客服:1413575084
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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
  • Leibniz-Institut für Pflanzenbiochemie (IPB) (Germany)
  • VIT University (India)
  • Institute of Tropical Disease Universitas Airlangga (Indonesia)
  • CSIRO - Agriculture Flagship (Australia)
  • Universiti Putra Malaysia(UPM) (Malaysia)
  • Seoul National University of Science and Technology (Korea)
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  • Massachusetts General Hospital (USA)
  • Institute of Bioorganic Chemistry Polish Academy of Sciences (Poland)
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  • Technical University of Denmark (Denmark)
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  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Tissue Cell.2024, 88:102401.
  • J of Health Science and Alternative Medicine2019, 1(1)
  • Toxins (Basel).2021, 13(9):593.
  • Front Chem.2022, 10:1048467.
  • J of Apicultural Research2020, 10.1080
  • Appl. Sci.2020, 10(16),5482.
  • Phytomedicine.2018, 47:48-57
  • Hanoi University of Pharmacy2023, 14(1):30-39.
  • Life Sci.2021, 286:120019.
  • Front Pharmacol.2021, 12:690113.
  • Trop J Nat Prod Res.2019, 3(1):6-9
  • J Biomed Sci.2020, 27(1):60.
  • Research Square2021, March 3rd.
  • Mediators Inflamm.2016, 2016:7216912
  • The Journal of Agromedicine and Medical Sciences2018, 4(1)
  • Molecules.2018, 23(11):E2837
  • Univerzita Karlova2021, 20.500.11956.
  • Applied Biological Chemistry2022, 65(85).
  • Life Sci.2023, 332:122107.
  • Nutr Res Pract.2020, 14(3):203-217.
  • Food Research International2020, 108987
  • J Agric Food Chem.2018, 66(1):351-358
  • J Microbiol Biotechnol.2020, 30(2):178-186.
  • ...
  • 生物活性
    Description: Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy.
    Targets: Src | Autophagy
    In vitro:
    Mol Cancer Res,2009 Apr;7(4):476-88.
    The Src inhibitor AZD0530 reversibly inhibits the formation and activity of human osteoclasts.[Pubmed: 19372577]
    Tumor cells in the bone microenvironment are able to initiate a vicious cycle of bone degradation by mobilizing osteoclasts, multinucleated cells specialized in bone degradation. c-Src is highly expressed both in tumors and in osteoclasts. Therefore, drugs like AZD0530, designed to inhibit Src activity, could selectively interfere with both tumor and osteoclast activity.
    METHODS AND RESULTS:
    Here we explored the effects of AZD0530 on human osteoclast differentiation and activity. The effect on osteoclasts formed in vivo was assessed in mouse fetal calvarial explants and in isolated rabbit osteoclasts, where it dose-dependently inhibited osteoclast activity. Its effect on formation and activity of human osteoclasts in vitro was determined in cocultures of human osteoblasts and peripheral blood mononuclear cells. AZD0530 was most effective in inhibiting osteoclast-like cell formation when present at the onset of osteoclastogenesis, suggesting that Src activity is important during the initial phase of osteoclast formation. Formation of active phosphorylated c-Src, which was highly present in osteoclast-like cells in cocultures and in peripheral blood mononuclear cell monocultures, was significantly reduced by AZD0530. Furthermore, it reversibly prevented osteoclast precursor migration from the osteoblast layer to the bone surface and subsequent formation of actin rings and resorption pits.
    CONCLUSIONS:
    These data suggest that Src is pivotal for the formation and activity of human osteoclasts, probably through its effect on the distribution of the actin microfilament system. The reversible effect of AZD0530 on osteoclast formation and activity makes it a promising candidate to temper osteoclastic bone degradation in bone diseases with enhanced osteoclast activity such as osteolytic metastatic bone disease.
    In vivo:
    Mol Oncol,2009 Jun;3(3):248-61.
    Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530.[Pubmed: 19393585]

    METHODS AND RESULTS:
    AZD0530, an orally available Src inhibitor, demonstrated potent antimigratory and anti-invasive effects in vitro, and inhibited metastasis in a murine model of bladder cancer. Antiproliferative activity of AZD0530 in vitro varied between cell lines (IC(50) 0.2 ->10μM). AZD0530 inhibited tumor growth in 4/10 xenograft models tested and dynamically inhibited in vivo phosphorylation of Src substrates paxillin and FAK in both growth-inhibition-resistant and -sensitive xenografts. The activity of AZD0530 in NBT-II bladder cancer cells in vitro was consistent with inhibition of cell migration and stabilization of cell-cell adhesion.
    CONCLUSIONS:
    These data suggest a dominant anti-invasive pharmacology for AZD0530 that may limit tumor progression in a range of cancers. AZD0530 is currently in Phase II clinical trials.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 1.8449 mL 9.2246 mL 18.4492 mL 36.8983 mL 46.1229 mL
    5 mM 0.369 mL 1.8449 mL 3.6898 mL 7.3797 mL 9.2246 mL
    10 mM 0.1845 mL 0.9225 mL 1.8449 mL 3.6898 mL 4.6123 mL
    50 mM 0.0369 mL 0.1845 mL 0.369 mL 0.738 mL 0.9225 mL
    100 mM 0.0184 mL 0.0922 mL 0.1845 mL 0.369 mL 0.4612 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
    (1R-反式)-2-甲酰基-4-羟基-3-甲基-alpha-亚甲基-2-环戊烯-1-乙醛; 8,9-Didehydro-7-hydroxydolichodial CFN96384 97856-19-4 C10H12O3 = 180.2 5mg QQ客服:2056216494
    艾希勒螺内酯; Eichlerialactone CFN98092 2202-01-9 C27H42O4 = 430.6 5mg QQ客服:2056216494
    Barbacarpan; Barbacarpan CFN98069 213912-46-0 C20H18O4 = 322.4 5mg QQ客服:1457312923
    N-丙二酰DL-色氨酸; N-Malonyl DL-tryptophan CFN70337 3184-74-5 C14H14N2O5 = 290.3 5mg QQ客服:3257982914

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