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硫酸长春碱 /Vinblastine sulfate {[allProObj[0].p_purity_real_show]}

货号:A346669 同义名: Vincaleukoblastine sulfate salt;Vinblastine (sulfate)

Vinblastine Sulfate is a natural product targeting on microtubule formation, and also inhibits nAChR with IC50 value of 8.9 μM.

Vinblastine sulfate 化学结构 CAS号:143-67-9
Vinblastine sulfate 化学结构
CAS号:143-67-9
Vinblastine sulfate 3D分子结构
CAS号:143-67-9
Vinblastine sulfate 化学结构 CAS号:143-67-9
Vinblastine sulfate 3D分子结构 CAS号:143-67-9
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Vinblastine sulfate 纯度/质量文件 产品仅供科研

货号:A346669 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AChE AChR mAChR nAChR 其他靶点 纯度
Donepezil +++

hAChE, IC50: 11.6 nM

bAChE, IC50: 8.12 nM

98%
Loganin ++

AChE, IC50: 3.95 μM

99%+
topride HCl ++

AChE, IC50: 2.04 μM

98%
Dehydroevodiamine HCl 99%+
Jatrorrhizine ++

AChE, IC50: 872 nM

99%+
Palmatine ++

AChE, IC50: 0.51 μM

98%
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

98%
Galanthamine HBr ++

AChE, IC50: 0.35 μM

98%
Trospium chloride 99%
Tiotropium Bromide Monohydrate 98+%
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

98%
Hexamethonium Bromide 99%
Pancuronium dibromide 98%
Neostigmine bromide 98%
Orphenadrine citrate 98%
Oxybutynin 98%
Irsogladine PDE 98%
Pyridostigmine bromide 99+%
Rivastigmine +

AChR, IC50: 5.5 μM

98%
Paroxetine hydrochloride 97%
Rocuronium Bromide 98%
Tropicamide +++

M4 mAChR, IC50: 8 nM

98%
Diphenmanil methylsulfate 98%
Umeclidinium bromide 95%
Otilonium bromide 98%
Flavoxate HCl +

mAChR, IC50: 12.2 μM

98%
Ipratropium bromide 98%
Diphenidol HCl 98%
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

98%
Aclidinium Bromide ++++

M4 mAChR, Ki: 0.21 nM

M2 mAChR, Ki: 0.1 nM

98%
Oxybutynin chloride 99%
Pentoxyverine citrate 98%
Solifenacin 98%
Catharanthine 98%
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

99+%
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

99%
PNU-120596 ++

α7 nAChR, EC50: 216 nM

99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Vinblastine sulfate 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].
体内研究

Vinblastine, an extensively utilized anticancer medication, is associated with undesirable side effects. Its conjugation with carrier molecules presents a potentially effective strategy for mitigating these adverse effects [5].

体外研究

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].

Vinblastine sulfate 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
ACHN cells Cytotoxicity assay 48 h Cytotoxicity against human ACHN cells after 48 hrs by SRB assay, IC50=22.7 μM 19467877

Vinblastine sulfate 动物研究

Dose Mice: 10 mg/kg[3] (median lethal dose, i.v.) Rat: 2.9 mg/kg[3] (median lethal dose, i.v.); 2.9 mg/kg[3] (median lethal dose, p.o.)
Administration i.v., p.o.

Vinblastine sulfate 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.

Vinblastine sulfate 实验方案

计算器
存储液制备 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

Vinblastine sulfate 技术信息

CAS号143-67-9
分子式C46H60N4O13S
分子量 909.053
别名 Vincaleukoblastine sulfate salt;Vinblastine (sulfate);VLB;Vincaleukoblastinesulfate;Velsar;Velban®;Rozevinsulfate;Exal;Alkaban-AQ;29060-LE;Vincaleukoblastine;NSC-49842
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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