Combretastatin A-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Combretastatin A-1 是一种微管聚合抑制剂，可与微管蛋白的秋水仙碱结合位点结合。Combretastatin A-1 通过微管蛋白解聚介导的 AKT 失活抑制 Wnt/β-catenin 通路。Combretastatin A-1 具有抗肿瘤和抗血管作用。

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.

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 (IC50=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..Western Blot Analysis Cell 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.

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.Animal Model:Male athymic BALB/c nu/nu mice (16-18 g; 4-6 weeks old) were inoculated with HepG2 cells Dosage: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.

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Others

Other Targets

Microtubule Associated | Akt

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109971-63-3

332.35

C18H20O6

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 100 mg/mL (300.89 mM )

COc1ccc(\C=C/c2cc(OC)c(OC)c(OC)c2)c(O)c1O

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(-20℃)

With Ice Pack

≥ 2 years