Vinblastine sulfate
(Synonyms: 硫酸长春碱; Vincaleukoblastine sulfate salt) 目录号 : GC12286
Vinblastine sulfate是一种细胞毒性生物碱。
Cas No.:143-67-9
Sample solution is provided at 25 µL, 10mM.
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Vinblastine sulfate is a cytotoxic alkaloid [1]. Vinblastine sulfate inhibits the proliferation of cancer cells by inhibiting the polymerization of tubulin (nAChR: IC50 = 8.9μM) and interfering with the formation of the spindle during cell division [2-3]. Vinblastine sulfate is used to treat several types of cancer (Hodgkin's lymphoma, non-small cell lung cancer, bladder cancer, brain cancer, melanoma, and testicular cancer) [4].
In human acute promyelocytic leukaemia (NB4) cells, Vinblastine sulfate (50μM; 19h) reduced NB4 cell viability in a time- and concentration-dependent manner and concurrently promoted apoptosis and cell cycle arrest [5]. In Caco-2 cells, completion of culture medium with Vinblastine sulfate (10nM; 19d) increased the P-gp mRNA and the expression at protein level [6]. In Hela cells, Vinblastine sulfate (1, 10, 100, 1000, 10000µg/mL; 24h, 48h) treatment inhibits the proliferation of HeLa cells, and its inhibitory effect increases in a dose-dependent manner [7].
In fibrosarcoma mouse model, Vinblastine sulfate (0.25, 0.5, 1.0, 2.0mg/kg; ip; single injection) treatment reduces the incidence of DNA strand breaks in fibrosarcomas, blood leukocytes, and bone marrow cells in mice in a dose-dependent manner [8]. In Swiss mice, Vinblastine sulfate (0.5, 1.0, 1.5mg/kg; ip; single injection) is clastogenic in mouse bone marrow [9].
References:
[1]. McKay DB, Burkman AM. Nicotinic and nonnicotinic receptor-mediated actions of vinblastine. Proceedings of the Society for Experimental Biology and Medicine. 1993 Jul; 203(3): 372-376.
[2]. Pandya P, Agarwal LK, Gupta N, et al. Molecular recognition pattern of cytotoxic alkaloid vinblastine with multiple targets. Journal of Molecular Graphics and Modelling. 2014 Nov 1; 54: 1-9.
[3]. Sui M, Fan W. Combination of γ-radiation antagonizes the cytotoxic effects of vincristine and vinblastine on both mitotic arrest and apoptosis. International Journal of Radiation Oncology* Biology* Physics. 2005 Mar 15; 61(4): 1151-1158.
[4]. Du GH, Zhang YW, Kong XY, et al. Vinblastine and vincristine. Natural Small Molecule Drugs from Plants. 2018: 551-557.
[5]. Calviño E, Tejedor MC, Sancho P, et al. JNK and NFκB dependence of apoptosis induced by vinblastine in human acute promyelocytic leukaemia cells. Cell Biochemistry and Function. 2015 Jun; 33(4): 211-219.
[6]. Hellinger É, Bakk ML, Pócza P, et al. Drug penetration model of vinblastine-treated Caco-2 cultures. European journal of pharmaceutical sciences. 2010 Sep 11; 41(1): 96-106.
[7]. Yasin YS, Jumaa AH, Jabbar S, et al. Effect of laetrile vinblastine combination on the proliferation of the hela cancer cell line. Asian Pacific Journal of Cancer Prevention: APJCP. 2023; 24(12): 4329.
[8]. Rajagopalan R, Ranjan SK, Nair CK. Effect of vinblastine sulfate on γ-radiation-induced DNA single-strand breaks in murine tissues. Mutation Research/Genetic Toxicology and Environmental Mutagenesis. 2003 Apr 20; 536(1-2): 15-25.
[9]. Choudhury RC, Palo AK, Padhy A. Cytogenetic consequences of vinblastine treatment in mouse bone marrow. Chemotherapy. 2004 Oct 29; 50(4): 171-177.
Vinblastine sulfate是一种细胞毒性生物碱 [1]。Vinblastine sulfate通过抑制微管蛋白聚合（nAChR：IC50 = 8.9μM）并干扰细胞分裂过程中纺锤体的形成来抑制癌细胞增殖 [2-3]。Vinblastine sulfate用于治疗多种癌症（霍奇金淋巴瘤、非小细胞肺癌、膀胱癌、脑癌、黑色素瘤和睾丸癌） [4]。
在人急性早幼粒细胞白血病（NB4）细胞中，Vinblastine sulfate（50μM；19h）以时间和浓度依赖性方式降低NB4细胞活力，同时促进细胞凋亡和细胞周期停滞 [5]。在Caco-2细胞中，用Vinblastine sulfate（10nM；19d）完成培养基培养可增加P-gp mRNA和蛋白质水平的表达 [6]。在HeLa细胞中，Vinblastine sulfate（1、10、100、1000、10000µg/mL；24h、48h）处理可抑制HeLa细胞增殖，且其抑制作用呈剂量依赖性增强 [7]。
在小鼠纤维肉瘤模型中，Vinblastine sulfate（0.25、0.5、1.0、2.0mg/kg；ip；单次注射）处理可剂量依赖性地降低小鼠纤维肉瘤、血液白细胞和骨髓细胞中DNA链断裂的发生率 [8]。在瑞士小鼠中，Vinblastine sulfate（0.5、1.0、1.5mg/kg；ip；单次注射）在小鼠骨髓中具有致染色体断裂作用 [9]。
| Cell experiment [1]: | |
Cell lines | Human acute promyelocytic leukaemia (NB4) cells |
Preparation Method | For all experiments, the cells were seeded in 12 well culture plates in regular culture medium at a density of 5×105cells/mL. Stock solutions of Vinblastine sulfate were prepared by dilution in dimethyl sulfoxide (DMSO). Cells were treated with different concentrations of Vinblastine sulfate for different times in culture medium. Each of the used reagents was diluted with culture medium to the desired concentration with a final DMSO concentration of 0.1%. DMSO was added to untreated cultures at 0.1% (v/v) as a solvent control. NB4 cells were treated with 50μM Vinblastine sulfate for 19h. All the treatments were performed at 37°C in 5% CO2. |
Reaction Conditions | 50μM; 19h |
Applications | Vinblastine sulfate reduced NB4 cell viability in a time- and concentration-dependent manner and concurrently promoted apoptosis and cell cycle arrest. |
| Animal experiment [2]: | |
Animal models | Fibrosarcoma mouse model |
Preparation Method | For studying the influence of Vinblastine sulfate on radiation-induced DNA strand breaks, a serially transplanted fibrosarcoma originally developed by subcutaneous injection of 6,12-dimethylbenzo[1,2b,5,4-b]dithionaphthene was used as test system. Fifteen-day-old tumours were excised, minced and single-cell suspensions were prepared. The viable single-cell suspension of murine fibrosarcoma (106 cells in 0.2mL saline) was transplanted by subcutaneous injection on the dorsal side of hind limbs of the mice. When the tumor was grown to a diameter of 6-8mm, the experiments were conducted. Animals were administered intraperitoneally with 0.0, 0.25, 0.5, 1.0 and 2.0mg/kg body weight of commercially available Vinblastine sulfate. |
Dosage form | 0.25, 0.5, 1.0, 2.0mg/kg; ip; single injection |
Applications | Vinblastine sulfate treatment reduces the incidence of DNA strand breaks in fibrosarcomas, blood leukocytes, and bone marrow cells in mice in a dose-dependent manner. |
References: | |
| Cas No. | 143-67-9 | SDF | |
| 别名 | 硫酸长春碱; Vincaleukoblastine sulfate salt | ||
| Canonical SMILES | CCC1(CC2CC(C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O.OS(=O)(=O)O | ||
| 分子式 | C46H60N4O13S | 分子量 | 909.05 |
| 溶解度 | ≥ 28.85 mg/mL in DMSO, ≥ 48.2 mg/mL in Water with ultrasonic | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1 mL | 5.5002 mL | 11.0005 mL |
| 5 mM | 0.22 mL | 1.1 mL | 2.2001 mL |
| 10 mM | 0.11 mL | 0.55 mL | 1.1 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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