Combretastatin A-1

小分子

考布他汀A-1

3-methoxy-6-[(E)-2-(3,4,5-trimethoxyphenyl)vinyl]benzene-1,2-diol | (Z)-3-METHOXY-6-(3,4,5-TRIMETHOXYSTYRYL)BENZENE-1,2-DIOL | Acetic acid n-amyl ester | MS-24999 | (Z)-3-(3,4,5-trimethoxystyryl)-6-methoxybenzene-1,2-diol | (Z)-2'',3''-dihydroxy-3,4,4'',5

Combretastatin A-1

C648131-5mg

5mg

≥97%

-20°C储存

超低温冰袋运输

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. Form:Solid IC50& Target:Microtubule/Tubulin

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

109971-63-3

C18H20O6

332.35 g/mol

5458993

COC1=C(C(=C(C=C1)/C=C\C2=CC(=C(C(=C2)OC)OC)OC)O)O

3-methoxy-6-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]benzene-1,2-diol

1S/C18H20O6/c1-21-13-8-7-12(16(19)17(13)20)6-5-11-9-14(22-2)18(24-4)15(10-11)23-3/h5-10,19-20H,1-4H3/b6-5-

YUSYSJSHVJULID-WAYWQWQTSA-N

COC1=C(C(=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)O)O

5458993

109971-63-3

combretastatin A-1;Combretastatin A1;NSC 600032;NSC-600032

DMSO : ≥ 100 mg/mL (300.89 mM)

2

6

6

332.126 Da

332.126 Da

77.400 Ų

24

0

387.000

0

1

3.400

600032