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Vinblastine sulfate

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Chemical Structure| 143-67-9 同义名 : Vincaleukoblastine sulfate salt;Vinblastine (sulfate);VLB;Vincaleukoblastinesulfate;Velsar;Velban®;Rozevinsulfate;Exal;Alkaban-AQ;29060-LE;Vincaleukoblastine;NSC-49842
CAS号 : 143-67-9
货号 : A346669
分子式 : C46H60N4O13S
纯度 : 99%
分子量 : 909.053
MDL号 : MFCD08706468
存储条件:

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 45 mg/mL(49.5 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(55 mM),配合低频超声助溶

动物实验配方:
生物活性
靶点
  • nAChR

    nAChR, IC50:8.9 μM

描述 Vinblastine, while not causing depolymerization of spindle microtubules, effectively blocks mitosis (e.g., IC50 0.8 nM in HeLa cells), leading to apoptotic cell death [2]. In NB4 cells, vinblastine induces alterations in p53 and DNA fragmentation. Its antiproliferative effect involves inducing apoptosis by disrupting the Bax/Bcl-2 balance. Vinblastine also suppresses NFκB expression and activity while activating JNK, resulting in apoptosis through a caspase-dependent pathway [3]. Vinblastine induces apoptosis, characterized by mitochondrial membrane potential loss, cytochrome c and apoptosis-inducing factor release, caspase-9 and caspase-3 activation, and Poly (ADP-ribose) Polymerase cleavage [4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
142BR cells Cytotoxicity assay 48 h Cytotoxicity against human 142BR cells after 48 hrs by SRB assay, IC50=37.6 μM 19467877
A375 cells Cytotoxicity assay 48 h Cytotoxicity against human A375 cells after 48 hrs by SRB assay, IC50=7.2 μM 19467877
A549 cells Proliferation assay 48 h Antiproliferative activity against human A549 cells after 48 hrs by MTS assay, IC50=2.36 μM 22546674
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.10mL

0.22mL

0.11mL

5.50mL

1.10mL

0.55mL

11.00mL

2.20mL

1.10mL

参考文献

[1]Pandya P, et al. Molecular recognition pattern of cytotoxic alkaloid vinblastine with multiple targets. J Mol Graph Model. 2014 Nov;54:1-9.

[2]Calvi?o E, et al. JNK and NFκB dependence of apoptosis induced by vinblastine in human acute promyelocytic leukaemia cells. Cell Biochem Funct. 2015 Jun;33(4):211-9.

[3]Selimovic D, et al. Vinblastine-induced apoptosis of melanoma cells is mediated by Ras homologous A protein (Rho A) via mitochondrial and non-mitochondrial-dependent mechanisms. Apoptosis. 2013 Aug;18(8):980-97.

[4]Bánóczi Z, et al. Synthesis and in vitro antitumor effect of vinblastine derivative-oligoarginine conjugates. Bioconjug Chem. 2010 Nov 17;21(11):1948-55.