Combretastatin A-1

CAS: 109971-63-3 货号: C655308 分子式: C18H20O6 分子量: 332.35 PubChem CID: 5458993
有货
级别和纯度: 10mM in DMSO
别名
考布他汀A-1
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
C655308-1ml
期货 Stock Image
¥1,100.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects

In Vitro

Combretastatin A-1 (72 h) inhibits the growth of various tumor cell lines in vitro, including HepG2, SMMC-7721, Hepa 1-6, LM-3, Bel-7402, Huh7, BGC-803, MDA-MB-231, MCF-7, A375, NCI-1975, CT-26, HT-29, A549 cells (IC 50 =9.2, 12.8, 32.9, 33.8, 38.4, 728.2, 12.2, 17.6, 46.0, 61.0, 256.3, 1075.0, 2082.0, 2247.0 nM, respectively). Combretastatin A-1 (1-10 nM; 24 h) induces apoptosis by microtubule depolymerization-induced AKT inactivation and the removal of GSK-3β inhibition in HepG2 cells. Combretastatin A-1 (1-50 nM; 6 h) decreases the mitochondrial membrane potential (MMP) of HepG2 cells. Combretastatin A-1 shows dose-dependently ROS accumulation in HepG2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HepG2 cells Concentration: 1, 5, 10 nM Incubation Time: 24 hours Result: Significantly decreased Mcl-1 expression, but the Bcl-2 level was unchanged. Reduced p-GSK 3β (Ser9) without altering total GSK-3β protein levels, indicating an activation of GSK-3β. Reduced AKT phosphorylation on Ser473 without an obvious change in the total AKT protein levels.

In Vivo

Combretastatin A-1 (1-4 mg/kg; i.v. every other day for 4 weeks) significantly reduces the tumor volume in HepG2 subcutaneous xenograft model. Combretastatin A-1 (2 mg/kg; every other day for 21 days) shows enhanced apoptosis in orthotopic hepatocellular carcinoma mouse model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male athymic BALB/c nu/nu mice (16-18 g; 4-6 weeks old) were inoculated with HepG2 cellsDosage: 1, 2, 4 mg/kg Administration: I.v. every other day for 4 weeks Result: Resulted in a significant tumor volume reduction at the dose of 2 mg/kg or 4 mg/kg.

IC50& Target:Microtubule/Tubulin

规格

别名
考布他汀A-1
规格或纯度
10mM in DMSO
英文名称
Combretastatin A-1
生化机理
Combretastatin A-1 是一种微管聚合抑制剂,能与小管蛋白的秋水仙碱结合位点结合。Combretastatin A-1 通过小管蛋白解聚介导的 AKT 失活抑制 Wnt/β-catenin 通路。考布他丁 A-1 具有以下特点
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
COC1=C(C(=C(C=C1)/C=C\C2=CC(=C(C(=C2)OC)OC)OC)O)O
关联CAS
PubChem CID
NSC Number
600032
MeSH Entry Terms
combretastatin A-1;Combretastatin A1;NSC 600032;NSC-600032
分子量
332.35

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