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  • 长春碱

    Vinblastine

    长春碱
    产品编号 CFN90230
    CAS编号 865-21-4
    分子式 = 分子量 C46H58N4O9 = 810.96
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Alkaloids
    植物来源 The herbs of Catharanthus roseus (L.)G. Don
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    长春碱 CFN90230 865-21-4 10mg QQ客服:1457312923
    长春碱 CFN90230 865-21-4 20mg QQ客服:1457312923
    长春碱 CFN90230 865-21-4 50mg QQ客服:1457312923
    长春碱 CFN90230 865-21-4 100mg QQ客服:1457312923
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    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.
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    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
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    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.
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    PMID: 28005066

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    IF=12.804(2019)

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  • ...
  • 生物活性
    Description: Vinblastine is a cytotoxic alkaloid used against various cancer types. Vinblastine inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.Vinblastine potently induced the proapoptotic protein PMAIP1 (NOXA) in both time- and dose-dependent manner and this was required for the observed apoptosis.The combination of antifungal azoles with Vinblastine can increase the incidence and severity of hyponatremia. Therefore, combined administration of azole antifungals with Vinblastine should be avoided.
    Targets: ATPase | PARP | Caspase | P450 (e.g. CYP17) | HSP (e.g. HSP90) | Calcium Channel | NF-kB | IkB | AP-1 | JNK | p38MAPK | IKK
    In vitro:
    Exp Parasitol. 2014 Nov;146:25-33.
    Leishmania amazonensis: Increase in ecto-ATPase activity and parasite burden of vinblastine-resistant protozoa.[Pubmed: 25176449]
    Leishmania amazonensis is a protozoan parasite that induces mucocutaneous and diffuse cutaneous lesions upon infection. An important component in treatment failure is the emergence of drug-resistant parasites. It is necessary to clarify the mechanism of resistance that occurs in these parasites to develop effective drugs for leishmaniasis treatment.
    METHODS AND RESULTS:
    Promastigote forms of L. amazonensis were selected by gradually increasing concentrations of Vinblastine and were maintained under continuous drug pressure (resistant cells). Vinblastine-resistant L. amazonensis proliferated similarly to control parasites. However, resistant cells showed changes in the cell shape, irregular flagella and a decrease in rhodamine 123 accumulation, which are factors associated with the development of resistance, suggesting the MDR phenotype. The Mg-dependent-ecto-ATPase, an enzyme located on cell surface of Leishmania parasites, is involved in the acquisition of purine and participates in the adhesion and infectivity process. We compared control and resistant L. amazonensis ecto-enzymatic activities. The control and resistant Leishmania ecto-ATPase activities were 16.0 ± 1.5 nmol Pi × h(-1) × 10(-7) cells and 40.0 ± 4.4 nmol Pi × h(-1) × 10(-7)cells, respectively. Interestingly, the activity of other ecto-enzymes present on the L. amazonensis cell surface, the ecto-5' and 3'-nucleotidases and ecto-phosphatase, did not increase. The level of ecto-ATPase modulation is related to the degree of resistance of the cell. Cells resistant to 10 μM and 60 μM of Vinblastine have ecto-ATPase activities of 22.7 ± 0.4 nmol Pi × h(-1) × 10(-7) cells and 33.8 ± 0.8 nmol Pi × h(-1) × 10(-7)cells, respectively. In vivo experiments showed that both lesion size and parasite burden in mice infected with resistant parasites are greater than those of L. amazonensis control cells. Furthermore, our data established a relationship between the increase in ecto-ATPase activity and greater infectivity and severity of the disease caused by Vinblastine-resistant L. amazonensis promastigotes.
    CONCLUSIONS:
    Taken together, these data suggest that ecto-enzymes could be potential therapeutic targets in the struggle against the spread of leishmaniasis, a neglected world-wide public health problem.
    In vivo:
    Int J STD AIDS. 2015 Mar;26(3):206-8.
    Autonomic neuropathy resulting in recurrent laryngeal nerve palsy in an HIV patient with Hodgkin lymphoma receiving vinblastine and antiretroviral therapy.[Pubmed: 24828552]
    Hoarseness of voice due to vocal cord paresis as a result of recurrent laryngeal nerve palsy has been well recognised. Recurrent laryngeal nerve palsy is commonly caused by compression due to tumour or lymph nodes or by surgical damage. Vinca alkaloids are well known to cause peripheral neuropathy. However, vinca alkaloids causing recurrent laryngeal nerve palsy has been reported rarely in children.
    METHODS AND RESULTS:
    We report a case of an adult patient with HIV who developed hoarseness of voice due to vocal cord paralysis during vinblastine treatment for Hodgkin lymphoma. Mediastinal and hilar lymph node enlargement in such patients may distract clinicians from considering alternative causes of recurrent laryngeal nerve palsy, with potential ensuing severe or even life-threatening stridor.
    Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2014 Oct;22(5):1386-90.
    Antifungal azoles exacerbate vinblastine-related hyponatremia in ALL children[Pubmed: 25338594]
    The purpose of this study was to investigate the clinical characteristics and the treatments of patients with vinblastine-related hyponatremia which was aggravated by azole antifungal agents in children with acute lymphoblastic leukemia(ALL).
    METHODS AND RESULTS:
    A total of 93 children treated with vinblastine in our department during April 2013 to March 2014 were enrolled in this study and were divided into 3 groups:VDLD, VDLD with azoles antifungal, VDLD with non azoles antifungal. The incidence and severity of hyponatremia were statistically analysed. The results showed that (1) the incidence of hyponatremia in VDLD group was 93.1%(67/72),100%(13/13) in VDLD with azoles antifungal group, and 75%(6/8) in VDLD with non-azoles antifungal, there was no statistically difference between these three groups. (2) Incidence of moderate to severe hyponatremia (Na<129 mmol/L) in VDLD with azoles antifungal group was(9/13,69.2%),which was significartly higher than those in VDLD group (22/72, 30.6%) and in VDLD with non azoles antifungal group (1/8, 12.5%). However, the difference between VDLD group and VDLD with non azoles antifungal group were not statistical significant. (3) the lowest serum sodium level in VDLD with azoles antifungal group (124.0 ± 8.6 mmol/L) was significantly lower than that in VDLD group (130.8 ± 3.8 mmol/L)and VDLD+non azoles antifungal group(132.9 ± 4.9 mmol/L). Otherwise, the difference was not statistically significant between VDLD group and VDLD with non azoles antifungal group. (4) four children with severe hyponatremia showed convulsions and coma which all belong to VDLD with azoles antifungal group. The children with hyponatremia were restricted intake of fluid, adjusted the liquid tension, supplied hypertonic sodium and given diuretic, the serum sodium value gradually picked up in these children. In 4-11 months' follow-up, no hyponatremia happened again in these children.
    CONCLUSIONS:
    It is concluded that the incident of hyponatremia in children treated with vinblastine is high, but most of them seldom showed clinical characteristics. The combination of antifungal azoles with vinblastine can increase the incidence and severity of hyponatremia. Therefore, combined administration of azole antifungals with vinblastine should be avoided.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 1.2331 mL 6.1655 mL 12.3311 mL 24.6621 mL 30.8277 mL
    5 mM 0.2466 mL 1.2331 mL 2.4662 mL 4.9324 mL 6.1655 mL
    10 mM 0.1233 mL 0.6166 mL 1.2331 mL 2.4662 mL 3.0828 mL
    50 mM 0.0247 mL 0.1233 mL 0.2466 mL 0.4932 mL 0.6166 mL
    100 mM 0.0123 mL 0.0617 mL 0.1233 mL 0.2466 mL 0.3083 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
    酒石酸长春瑞滨; Vinorelbine Tartrate CFN90142 125317-39-7 C53H66N4O20 = 1079.11 20mg QQ客服:1457312923
    硫酸长春碱; Vinblastine Sulfate CFN90146 143-67-9 C46H58N4O9.H2SO4 = 909.06 20mg QQ客服:1413575084
    长春碱; Vinblastine CFN90230 865-21-4 C46H58N4O9 = 810.96 20mg QQ客服:215959384
    脱水长春碱; 3',4'-Anhydrovinblastine CFN90246 38390-45-3 C46H56N4O8 = 792.96 5mg QQ客服:215959384
    硫酸长春新碱; Vincristine sulfate CFN90400 2068-78-2 C46H58N4O14S = 923.04 20mg QQ客服:3257982914
    长春瑞滨; Vinorelbine CFN90401 71486-22-1 C45H54N4O8 = 778.93 20mg QQ客服:215959384
    长春地辛; Vindesine CFN90465 53643-48-4 C43H55N5O7 = 753.92 5mg QQ客服:215959384
    环氧长春碱,长春素; Vinleurosine CFN90466 23360-92-1 C46H56N4O9 = 808.95 5mg QQ客服:1457312923
    长春新碱; Vincristine CFN98589 57-22-7 C46H56N4O10 = 824.96 20mg QQ客服:3257982914

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