Vinblastine sulfate

别名: NSC-49842, Vincaleukoblastine, 29060-LE 中文名称：硫酸长春碱

目录号：S4505 Purity: 99.91%

Vinblastine sulfate抑制微管形成和nAChR活性，在无细胞实验的测定中，IC50为8.9 μM。Vinblastine sulfate 可诱导自噬和凋亡。

Vinblastine sulfate Chemical Structure

CAS: 143-67-9

规格	价格	库存
10mM (1mL in DMSO)	794.43	现货
5mg	573.88	现货
25mg	2023.45	现货
100mg	5545.08	现货
1g	20230.26	现货
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产品质控

批次：纯度： 99.91%

99.91

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细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
rat REF52 cells	Function assay	0.1 μM	30 mins	Induction of microtubule depolymerization in rat REF52 cells at 0.1 uM after 30 mins by fluorescence assay	23947826
K562 cell	Proliferation assay		48 h	Antiproliferative activity against human K562 cells after 48 hrs, IC50=0.001 μM	19220018
ACHN cells	Cytotoxicity assay		48 h	Cytotoxicity against human ACHN cells after 48 hrs by SRB assay, IC50=22.7 μM	19467877
A375 cells	Cytotoxicity assay		48 h	Cytotoxicity against human A375 cells after 48 hrs by SRB assay, IC50=7.2 μM	19467877
C32 cells	Cytotoxicity assay		48 h	Cytotoxicity against human C32 cells after 48 hrs by SRB assay, IC50=3 μM	19467877
LNCAP cells	Cytotoxicity assay		48 h	Cytotoxicity against human LNCAP cells after 48 hrs by SRB assay, IC50=29.3 μM	19467877
Huh-7D12 cells	Cytotoxicity assay		48 h	Cytotoxicity against human Huh-7D12 cells after 48 hrs by SRB assay, IC50=45.6 μM	19467877
COR-L23 cells	Cytotoxicity assay		48 h	Cytotoxicity against human COR-L23 cells after 48 hrs by SRB assay, IC50=45.5 μM	19467877
142BR cells	Cytotoxicity assay		48 h	Cytotoxicity against human 142BR cells after 48 hrs by SRB assay, IC50=37.6 μM	19467877
HT-29 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HT-29 cells after 48 hrs by MTS assay, IC50=0.55 μM	21920762
A549 cells	Proliferation assay		48 h	Antiproliferative activity against human A549 cells after 48 hrs by MTS assay, IC50=2.36 μM	22546674
DU145 cells	Proliferation assay		48 h	Antiproliferative activity against human DU145 cells after 48 hrs by MTS assay, IC50=4.25 μM	22546674
SK-MEL-5 cells	Proliferation assay		48 h	Antiproliferative activity against human SK-MEL-5 cells after 48 hrs by MTS assay, IC50=1.74 μM	22546674
HepG2 cells	Proliferation assay		48 h	Antiproliferative activity against human HepG2 cells after 48 hrs by MTS assay, IC50=0.16 μM	22546674
HT-29 cells	Proliferation assay		48 h	Antiproliferative activity against human HT-29 cells after 48 hrs by MTS assay, IC50=11.18 μM	22546674
MCF7 cells	Proliferation assay		48 h	Antiproliferative activity against human MCF7 cells after 48 hrs by MTS assay, IC50=24.08 μM	22546674
MDA-MB-231 cells	Proliferation assay		48 h	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTS assay, IC50=31.52 μM	22546674
HepG2 cells	Cytotoxicity assay		72 h	Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.056 μM	23708010
HepG2 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.019 μM	23708010
K562 cells	Cytotoxicity assay		72 h	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.016 μM	23708010
MDA-MB-231 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.0083 μM	23708010
MCF7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.007 μM	23708010
UACC903 cells	Cytotoxicity assay		48 h	Cytotoxicity against human UACC903 cells after 48 hrs by MTS assay, IC50=1.65 μM	21920762
BxPC3 cells	Proliferation assay		48 h	Antiproliferative activity against human BxPC3 cells after 48 hrs by MTS assay, IC50=1.13 μM	22546674
COLO 320 human colorectal carcinoma cell line	Function assay			In vitro concentration required to kill 50% of COLO 320 human colorectal carcinoma cell line, EC50=0.08 μM	12361397
LNCaP human prostate cancer cell line	Function assay			In vitro concentration required to kill 50% of LNCaP human prostate cancer cell line, EC50=0.5 μM	12361397
K562 cell	Growth inhibition assay			In vitro inhibitory concentration against human chronic myelogenous leukemia K562 cell growth, IC50=0.001 μM	12852768
T47D cells	Function assay			In vitro concentration required to kill 50% of T47D human breast ductal carcinoma cell line, EC50=0.08 μM	12361397
SCL6 cells	Cytotoxicity assay			Cytotoxicity against human SCL6 cells by MTT assay, ED50=6.1 Μm	12880314
SCL9	Cytotoxicity assay			Cytotoxicity against human SCL9 cells by MTT assay, ED=5.3 μM	12880314
KATO III cells	Cytotoxicity assay			Cytotoxicity against human KATO III cells by MTT assay, ED50=6.1 μM	12880314
NUGC4 cells	Cytotoxicity assay			Cytotoxicity against human NUGC4 cells by MTT assay, ED50=5.3 μM	12880314
K562 cells	Function assay			Inhibition of tubulin polymerization in human K562 cells, IC50=0.13 μM	20546980
点击查看更多细胞系数据

生物活性

产品描述

Vinblastine sulfate抑制微管形成和nAChR活性，在无细胞实验的测定中，IC50为8.9 μM。Vinblastine sulfate 可诱导自噬和凋亡。

靶点

nAChR ^[1]
(Adrenal Chromaffin Cells)

8.9 μM

体外研究(In Vitro)
体外研究活性	Vinblastine的平均终末半衰期为14.3小时。Vinblastine加入到新鲜分离的大鼠肝细胞，可迅速穿透到细胞当中^[3]。Vinblastine抑制由肾上腺髓质素诱导的血管生成反应，还可引起M期阻滞^[4]。在特定浓度下，vinblastine能显著增加微核单核细胞的数量^[2]。
细胞实验	细胞系	中国仓鼠卵巢细胞(CHO)
	浓度	1% (v/v) (dissolved in DMSO)
	孵育时间	3 h
	方法	6孔细胞培养板，每孔细胞密度为5×10⁴ cells/mL，悬浮于3 mL培养基中。向其中加入vinblastine孵育3小时，生长21小时后进行后续检测。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	ERK / p-ERK / Mcl-1 / Bad / Bid / Noxa p-JNK / c-Caspase-7 / c-PARP p-eIF2 GRP78		20371726
	Immunofluorescence	α-tubulin / Acetyl tubulin		30120268
	Growth inhibition assay	Cell viability		27114800

体内研究(In Vivo)
体内研究活性	Vinblastine作为抗癌剂被广泛运用，但具有一些意外的副作用^[6]。Vinblastine和RAP在低浓度下的结合使用，可在体内得到比较满意的抗血管形成作用^[4]。在临床使用剂量下，vinblastine抑制CEM细胞中的微管蛋白的棕榈酰化^[5]。

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06381570	Recruiting	Low-grade Glioma	Daniel Morgenstern\|The Hospital for Sick Children	March 21 2024	Early Phase 1

参考文献
[1] McKay DB, et al. Proc Soc Exp Biol Med. 1993, 203(3):372-376. [2] George E. Johnson, et al. Mutat Res. 2010, 702(2):189-192. [3] Zhou XJ, et al. Eur J Drug Metab Pharmacokinet. 1990, 15(4):323-332. [4] Ribatti D, et al. Oncogene. 2003, 22(41):6458-6461. [5] Joan M. Caron, et al. Chemotherapy. 2007, 53:51-58. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	909.05	分子式	C₄₆H₅₈N₄O₉.H₂SO₄
CAS号	143-67-9	SDF	Download Vinblastine sulfate SDF
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
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 100 mg/mL ( (110.0 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : 50 mg/mL (55.0 mM)

Ethanol : Insoluble

DMSO : 100 mg/mL ( (110.0 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

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 μL 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Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

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，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

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 ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：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。

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