ICM1035- Vinblastine sulfate

【英文同义名】：29060-LE, Vincaleucoblastine sulfate, VLB sulfate, Nincaluicolflastine, Vinblastine hydrogen sulfate, Velban®, Velsar®, Velbe®, Alkaban-AQ®, Exal®

【中文同义名】：硫酸长春碱

订购信息：（原装进口，常备现货）

品牌	产品名称	产品货号	规格	目录价（元）
Gene Operation	TW-37	ICM1035-0005MG	5 mg	¥839.00
		ICM1035-0010MG	10 mg	¥1,389.00
		ICM1035-0025MG	25 mg	¥2,629.00
		ICM1035-0050MG	50 mg	¥5,189.00

产品描述

硫酸长春碱是长春碱的硫酸盐形式,是从夹竹桃科植物长春花中提取的一种有抗癌活性的生物碱。主要抑制微管蛋白的聚合，抑制nAChR活性(IC₅₀=8.9)而妨碍纺锤体微管的形成，使有丝分裂停止于中期。在长春碱的作用中GDP的效果是GTP的3-5倍^[1-3]。长春花碱抑制稳态微管蛋白除了微管(Ki = 0.178±0.025μM),抑制B16黑素瘤细胞增殖(IC₅₀= 1nM),并在40 nM对L-细胞的生长产生完全的抑制^[1]。VLB在G2 / M期细胞周期阻断有丝分裂纺锤体的形成和随后引起细胞死亡的凋亡。长春碱可能是通过介导Bcl-2的***酸化，导致Bcl-2失活,并通过激活caspase-3来诱导细胞凋亡^[4]。长春花碱也可以抑制肾上腺皮质素刺激的血管生成响应在体外和体内^[5]。据报道, 长春花碱是某些癌症化疗方案中的一个有效的部分,特别是和博来霉素或甲氨蝶呤联合使用治疗 IA期VBM或IIA期的霍奇金淋巴瘤^[6]。硫酸长春花碱广泛用作抗微观药物治疗多种癌症,包括霍奇金淋巴瘤、非小细胞肺癌、乳腺癌、头颈部癌、睾丸癌和朗格汉斯细胞组织细胞增生症。

靶点

Targets	Microtubule/nAChR
IC₅₀	8.9 μM

化学特性

Cas No.: 143-67-9	分子量: 909.05
分子式: C₄₆H₅₈N₄O₉•H₂SO₄	纯度: >96%
同义名: 29060-LE, Vincaleucoblastine sulfate, VLB sulfate, Nincaluicolflastine, Vinblastine hydrogen sulfate, Velban®, Velsar®, Velbe®, Alkaban-AQ®, Exal®
化学名: dimethyl(2β,3β,4β,5α,12β,19α)-15-[(5S,9S)-5-ethyl-5-hydroxy-9-(methoxycarbonyl)-1,4,5,6,7,8,9,10- octahydro-2H-3,7-methanoazacycloundecino[5,4-b]indol-9-yl]-3-hydroxy-16-methoxy-1- methyl-6,7 -didehydroaspidospermidine- 3,4-dicarboxylate sulfate
外观: White to off-white solid
溶解度: Soluble in water (10 mg/mL) and DMSO (10 mg/mL). Poorly soluble in ethanol.
保存：Store solid at -20 ºC for the stability of two years.

储存液配制

储存液 (1 ml DMSO体系)	1 mM	5 mM	10 mM	25 mM	50 mM
质量(mg)	0.909	4.545	9.09	22.725	45.45

结构式

使用浓度(仅作参考)

Vinblastine sulfate的具体使用浓度请参考相关文献，并根据自身实验条件（如实验目的，细胞种类，培养特性等）进行摸索和优化。

参考文献

[1] Jordan MA, et al. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepi- dine on microtubule dynamics and cell proliferation in vitro. Cancer Res. 45(6):2741-7 (1985).

[2] Lobert S, et al. Interaction of vinca alkaloids with tubulin: a comparison of vinblastine, vincristine, and vinorelbine. Biochemistry. 35(21):6806-14 (1996).

[3] Gigant B, et al. Structural basis for the regulation of tubulin by vinblastine. Nature. 435(7041): 519-22 (2005).

[4] Tashiro E, et al. Caspase-3 activation is not responsible for vinblastine-induced Bcl-2 phosphorylation and G2/M arrest in human small cell lung carcinoma Ms-1 cells. Jpn J Cancer Res. 89(9):940-6 (1998).

[5] Ribatti D, et al. Vinblastine inhibits the angiogenic response induced by adrenomedullin in vitro and in vivo. Oncogene 22(41):6458–61 (2003).

[6] Gobbi PG, et al. Vinblastine, bleomycin, and methotrexate chemotherapy plus irradiation for patients with early-stage, favorable Hodgkin lymphoma: the experience of the Gruppo Italiano Studio Linfomi. Cancer. 98(11):2393-401 (2003).

同义名: 29060-LE, Vincaleucoblastine sulfate, VLB sulfate, Nincaluicolflastine, Vinblastine hydrogen sulfate, Velban®, Velsar®, Velbe®, Alkaban-AQ®, Exal®

外观: White to off-white solid