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  • 布帕尼西

    Buparlisib (BKM120)

    布帕尼西
    产品编号 CFN60065
    CAS编号 944396-07-0
    分子式 = 分子量 C18H21F3N6O2 = 410.39
    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
    布帕尼西 CFN60065 944396-07-0 1mg QQ客服:215959384
    布帕尼西 CFN60065 944396-07-0 5mg QQ客服:215959384
    布帕尼西 CFN60065 944396-07-0 10mg QQ客服:215959384
    布帕尼西 CFN60065 944396-07-0 20mg QQ客服:215959384
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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
  • Melbourne University (Australia)
  • Ain Shams University (Egypt)
  • University of Helsinki (Finland)
  • Utrecht University (Netherlands)
  • Centrum Menselijke Erfelijkheid (Belgium)
  • Mahatma Gandhi University (India)
  • National Hellenic Research Foundation (Greece)
  • Shanghai Institute of Organic Chemistry (China)
  • Universidade Federal de Santa Catarina (Brazil)
  • China Medical University (Taiwan)
  • Institute of Bioorganic Chemistry Polish Academy of Sciences (Poland)
  • National Research Council of Canada (Canada)
  • Celltrion Chemical Research Institute (Korea)
  • CSIRO - Agriculture Flagship (Australia)
  • More...
  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Processes2021, 9(11),2065.
  • Biochem Systematics and Ecology2017, 11-18
  • J Agric Food Chem.2024, 72(15):8784-8797.
  • J Cell Mol Med . 2023, jcmm.17954.
  • Chengdu University of Traditional Chinese Medicine2024, 4802935.
  • Neurochem Int.2023, 167:105537.
  • Emirates Journal of Food and Agriculture.2022, 34(6): 528-536.
  • Front Microbiol.2019, 10:2806
  • Planta Med.2016, 82(13):1208-16
  • Sci Rep. 2018, 462(8)
  • Nat Prod Sci.2016, 22(2)
  • Front Chem.2023, 11:1245071.
  • Biomed Pharmacother.2024, 176:116765.
  • Analytical Letters 2021, 54(4).
  • Phytomedicine.2023, 117:154929.
  • Sci Rep.2021, 11(1):21038.
  • Molecules.2021, 26(4):1084.
  • Environ Toxicol.2023, 38(7):1641-1650.
  • Horticulturae2021, 7(1),5.
  • The Journal of Supercritical Fluids2021, 176:105305.
  • Journal of Functional Foods2023, 104:105542
  • Food Chem.2023, 427:136647.
  • Molecules.2023, 28(16):6025.
  • ...
  • 生物活性
    Description: Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis.
    Targets: PI3K
    In vitro:
    J Mol Med (Berl),2012 Jun;90(6):695-706.
    Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity with dexamethasone.[Pubmed: 22207485]
    NVP-BKM120 is a novel phosphatidylinositol 3-kinase (PI3K) inhibitor and is currently being investigated in phase I clinical trials in solid tumors. This study aimed to evaluate the therapeutic efficacy of BKM120 in multiple myeloma (MM).
    METHODS AND RESULTS:
    BKM120 induces cell growth inhibition and apoptosis in both MM cell lines and freshly isolated primary MM cells. However, BKM120 only shows limited cytotoxicity toward normal lymphocytes. The presence of MM bone marrow stromal cells, insulin-like growth factor, or interleukin-6 does not affect BKM120-induced tumor cell apoptosis. More importantly, BKM120 treatment significantly inhibits tumor growth in vivo and prolongs the survival of myeloma-bearing mice. In addition, BKM120 shows synergistic cytotoxicity with dexamethasone in dexamethasone-sensitive MM cells. Low doses of BKM120 and dexamethasone, each of which alone has limited cytotoxicity, induce significant cell apoptosis in MM.1S and ARP-1. Mechanistic study shows that BKM120 exposure causes cell cycle arrest by upregulating p27 (Kip1) and downregulating cyclin D1 and induces caspase-dependent apoptosis by downregulating antiapoptotic XIAP and upregulating expression of cytotoxic small isoform of Bim, BimS.
    CONCLUSIONS:
    In summary, our findings demonstrate the in vitro and in vivo anti-MM activity of BKM120 and suggest that BKM120 alone or together with other MM chemotherapeutics, particularly dexamethasone, may be a promising treatment for MM.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.4367 mL 12.1835 mL 24.3671 mL 48.7341 mL 60.9177 mL
    5 mM 0.4873 mL 2.4367 mL 4.8734 mL 9.7468 mL 12.1835 mL
    10 mM 0.2437 mL 1.2184 mL 2.4367 mL 4.8734 mL 6.0918 mL
    50 mM 0.0487 mL 0.2437 mL 0.4873 mL 0.9747 mL 1.2184 mL
    100 mM 0.0244 mL 0.1218 mL 0.2437 mL 0.4873 mL 0.6092 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
    5,5'-二甲氧基开环异落叶松树脂酚; 5,5'-Dimethoxysecoisolariciresinol CFN92963 1002106-91-3 C22H30O8 = 422.47 5mg QQ客服:2056216494
    7,9,12-三羟基-2,2-二甲基-2H,6H-吡喃并[3,2-b]氧杂蒽-6-酮; O-Demethylforbexanthone CFN97493 92609-77-3 C18H14O6 = 326.3 5mg QQ客服:3257982914
    1-苯基乙基 beta-D-吡喃葡萄糖苷; 1-Phenylethyl beta-D-glucoside CFN95574 93199-03-2 C14H20O6 = 284.3 5mg QQ客服:2159513211
    Coromandaline; Coromandaline CFN00332 68473-86-9 C15H27NO4 = 285.38 5mg QQ客服:215959384

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