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  • 高三尖杉酯碱

    Homoharringtonine

    高三尖杉酯碱
    产品编号 CFN98110
    CAS编号 26833-87-4
    分子式 = 分子量 C29H39NO9 = 545.61
    产品纯度 >=98%
    物理属性 Cryst.
    化合物类型 Alkaloids
    植物来源 The branches of Cephalotaxus fortunei Hook.f.
    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
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    产品名称 产品编号 CAS编号 包装 QQ客服
    高三尖杉酯碱 CFN98110 26833-87-4 10mg QQ客服:215959384
    高三尖杉酯碱 CFN98110 26833-87-4 20mg QQ客服:215959384
    高三尖杉酯碱 CFN98110 26833-87-4 50mg QQ客服:215959384
    高三尖杉酯碱 CFN98110 26833-87-4 100mg 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
  • Calcutta University (India)
  • University of Vigo (Spain)
  • Shanghai University of TCM (China)
  • Rio de Janeiro State University (Brazil)
  • Weizmann Institute of Science (Israel)
  • Washington State University (USA)
  • University of Bonn (Germany)
  • Ain Shams University (Egypt)
  • Subang Jaya Medical Centre (Malaysia)
  • Sant Gadge Baba Amravati University (India)
  • University of British Columbia (Canada)
  • Lodz University of Technology (Poland)
  • Medical University of South Carolina (USA)
  • Agricultural Research Organization (ARO) (Israel)
  • More...
  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • J Sep Sci.2021, 44(22):4064-4081.
  • Int J Mol Med.2015, 35(5):1237-45
  • Korean j.of Pharm.2017, 70-76
  • Int Immunopharmacol. 2020, 83:106403.
  • ACS Pharmacol. Transl. Sci.2023, 3c00129.
  • Nat Prod Sci.2018, 24(3):206
  • Molecules.2021, 26(6):1738.
  • Pak J Pharm Sci.2019, 32(6):2879-2885
  • Agronomy2020, 10(3),388.
  • Yakugaku Zasshi.2018, 138(4):571-579
  • Exp Mol Med.2020, 52(4):629-642.
  • Molecules.2020, 25(7):1625.
  • Molecules.2022, 27(7):2093.
  • J Herbmed Pharmacol.2018, 7(4):280-286
  • Pharmacognosy Magazine2017, 13(52):868-874
  • Korean Herb. Med. Inf.2020, 8(2):243-254.
  • Front Immunol.2018, 9:2655
  • Biochem Biophys Res Commun.2018, 505(1):261-266
  • Plants (Basel).2021, 10(11):2525.
  • Nutrients.2020, 12(11):3448.
  • Int J Mol Sci.2019, 20(21):E5488
  • Foods.2021, 10(11):2754.
  • J.Food Processing & Preservation2022, jfpp.16666
  • ...
  • 生物活性
    Description: Homoharringtonine, a plant alkaloid with antitumor and antileukemic properties, inhibit protein translation by preventing the initial elongation step of protein synthesis via an interaction with the ribosomal A-site. Homoharringtonine might have clinical activity in some patients with myelodysplastic syndrome.
    Targets: Caspase | PARP | Bcl-2/Bax | MEK | ERK
    In vitro:
    Am J Hematol. 2004 Jul;76(3):199-204.
    Homoharringtonine mediates myeloid cell apoptosis via upregulation of pro-apoptotic bax and inducing caspase-3-mediated cleavage of poly(ADP-ribose) polymerase (PARP).[Pubmed: 15224352 ]
    Homoharringtonine (HHT) is a plant alkaloid with antileukemia activity that is currently being used for treatment of acute, chronic leukemias and MDS.
    METHODS AND RESULTS:
    In this study, we show that HHT can induce apoptosis in a variety of human myeloid leukemia cell lines (U937, HL-60, HEL, THP, and K562). U937 and HL60 cells undergo rapid apoptosis on treatment with HHT, as indicated by increased annexin V binding capacity, caspase-3 activation, and cleavage of poly(ADP-ribose) polymerase (PARP). In addition, the expression of bax is upregulated during HHT-induced cell death, whereas the expression of bcl-2 is only slightly decreased. Importantly, treatment of primary leukemic cells, obtained from acute myeloid leukemia patients, resulted in rapid apoptosis.
    CONCLUSIONS:
    Thus, our data provide the mechanism of HHT and justify the use of HHT in the treatment of human myeloid leukemia.
    Sci Rep. 2015 Jul 13;5:8477.
    Homoharringtonine induces apoptosis and inhibits STAT3 via IL-6/JAK1/STAT3 signal pathway in Gefitinib-resistant lung cancer cells.[Pubmed: 26166037]
    Tyrosine kinase inhibitors (TKIs) are mostly used in non-small cell lung cancer (NSCLC) treatment. Unfortunately, treatment with Gefitinib for a period of time will result in drug resistance and cause treatment failure in clinic.
    METHODS AND RESULTS:
    Therefore, exploring novel compounds to overcome this resistance is urgently required. Here we investigated the antitumor effect of homoharringtonine (HHT), a natural compound extracted from Cephalotaxus harringtonia, on Gefitinib-resistant NSCLC cell lines in vitro and in vivo. NCI-H1975 cells with EGFR T790M mutation are more sensitive to HHT treatment compared with that of A549 cells with wild type EGFR. HHT inhibited cells growth, cell viability and colony formation, as well as induced cell apoptosis through mitochondria pathway. Furthermore, we explored the mechanism of HHT inhibition on NSCLC cells. Higher level of interleukin-6 (IL-6) existed in lung cancer patients and mutant EGFR and TGFβ signal requires the upregulation of IL-6 through the gp130/JAK pathway to overactive STAT3, an oncogenic protein which has been considered as a potential target for cancer therapy. HHT reversiblely inhibited IL-6-induced STAT3 Tyrosine 705 phosphorylation and reduced anti-apoptotic proteins expression. Gefitinib-resistant NSCLC xenograft tests also confirmed the antitumor effect of HHT in vivo.
    CONCLUSIONS:
    Consequently, HHT has the potential in Gefitinib-resistant NSCLC treatment.
    In vivo:
    Lancet Oncol. 2013 Jun;14(7):599-608.
    Homoharringtonine-based induction regimens for patients with de-novo acute myeloid leukaemia: a multicentre, open-label, randomised, controlled phase 3 trial.[Pubmed: 23664707]
    Homoharringtonine-based induction regimens have been widely used in China for patients with acute myeloid leukaemia. However, their efficacy has not been tested in a multicentre randomised controlled trial in a large population. We assessed the efficacy and safety of homoharringtonine-based induction treatment for management of newly diagnosed acute myeloid leukaemia.
    METHODS AND RESULTS:
    This open-label, randomised, controlled, phase 3 study was done in 17 institutions in China between September, 2007, and July, 2011. Untreated patients aged 14-59 years with acute myeloid leukaemia were randomly assigned (by a computer-generated allocation schedule without stratification) to receive one of three induction regimens in a 1:1:1 ratio: homoharringtonine 2 mg/m(2) per day on days 1-7, cytarabine 100 mg/m(2) per day on days 1-7, and aclarubicin 20 mg/day on days 1-7 (HAA); homoharringtonine 2 mg/m(2) per day on days 1-7, cytarabine 100 mg/m(2) per day on days 1-7, and daunorubicin 40 mg/m(2) per day on days 1-3 (HAD); or daunorubicin 40-45 mg/m(2) per day on days 1-3 and cytarabine 100 mg/m(2) per day on days 1-7 (DA). Patients in complete remission were offered two cycles of intermediate-dose cytarabine (2 g/m(2) every 12 h on days 1-3). The primary endpoints were the proportion of patients who achieved complete remission after two cycles of induction treatment and event-free survival in the intention-to-treat population. The trial is registered in the Chinese Clinical Trial Register, number ChiCTR-TRC-06000054. We enrolled 620 patients, of whom 609 were included in the intention-to-treat analysis. 150 of 206 patients (73%) in the HAA group achieved complete remission versus 125 of 205 (61%) in the DA group (p=0.0108); 3-year event-free survival was 35.4% (95% CI 28.6-42.2) versus 23.1% (95% CI 17.4-29.3; p=0.0023). 133 of 198 patients (67%) in the HAD group had complete remission (vs DA, p=0·20) and 3-year event-free survival was 32.7% (95% CI 26.1-39.5; vs DA, p=0.08). Adverse events were much the same in all groups, except that more patients in the HAA (12 of 206 [5.8%]) and HAD (13 of 198 [6.6%]) groups died within 30 days than in the DA group (two of 205 [1%]; p=0.0067 vs HAA; p=0.0030 vs HAD).
    CONCLUSIONS:
    A regimen of homoharringtonine, cytarabine, and aclarubicin is a treatment option for young, newly diagnosed patients with acute myeloid leukaemia.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 1.8328 mL 9.1641 mL 18.3281 mL 36.6562 mL 45.8203 mL
    5 mM 0.3666 mL 1.8328 mL 3.6656 mL 7.3312 mL 9.1641 mL
    10 mM 0.1833 mL 0.9164 mL 1.8328 mL 3.6656 mL 4.582 mL
    50 mM 0.0367 mL 0.1833 mL 0.3666 mL 0.7331 mL 0.9164 mL
    100 mM 0.0183 mL 0.0916 mL 0.1833 mL 0.3666 mL 0.4582 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
    桥氧三尖杉碱; Drupacine CFN96761 49686-57-9 C18H21NO5 = 331.36 5mg QQ客服:2159513211
    三尖杉碱; Cephalotaxine CFN90919 24316-19-6 C18H21NO4 = 315.4 20mg QQ客服:1413575084
    4-羟基三尖杉碱; 4-Hydroxycephalotaxine CFN97338 84567-08-8 C18H21NO5 = 331.4 5mg QQ客服:1457312923
    乙酰三尖杉碱; Acetylcephalotaxine CFN98255 24274-60-0 C20H23NO5 = 357.4 5mg QQ客服:3257982914
    高三尖杉酯碱; Homoharringtonine CFN98110 26833-87-4 C29H39NO9 = 545.61 20mg QQ客服:2056216494
    三尖杉酯碱; Harringtonine CFN90891 26833-85-2 C28H37NO9 = 531.6 5mg QQ客服:2159513211
    Cephalocyclidin A; Cephalocyclidin A CFN98660 421583-14-4 C17H19NO5 = 317.3 5mg QQ客服:1413575084
    去甲基三尖杉碱; Demethylcephalotaxinone CFN96766 51020-45-2 C17H17NO4 = 299.32 5mg QQ客服:3257982914
    Chilenine; Chilenine CFN89525 71700-15-7 C20H17NO7 = 383.35 5mg QQ客服:1413575084

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