2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. Combretastatin A-1 phosphate tetrasodium

Combretastatin A-1 phosphate tetrasodium  (Synonyms: OXi-4503 tetrasodium)

目录号: HY-16146
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摩尔计算器

Combretastatin A-1 phosphate (OXi-4503) 是 Combretastatin A-1 的前体，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 phosphate tetrasodium 通过微管蛋白解聚介导的 AKT 失活抑制 Wnt/β-catenin 通路。Combretastatin A-1 phosphate tetrasodium 具有抗肿瘤和抗血管作用。

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Combretastatin A-1 phosphate tetrasodium Chemical Structure

Combretastatin A-1 phosphate tetrasodium Chemical Structure

CAS No. : 288847-34-7

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Combretastatin A-1 phosphate tetrasodium 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

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生物活性

Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a proagent of Combretastatin A-1, is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 phosphate tetrasodium exhibits anti-tumor and anti-vascular effects[1][2][3].

IC50 & Target

Microtubule/Tubulin[1]
体外研究
(In Vitro)

Combretastatin A-1 phosphate (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)[2].
Combretastatin A-1 phosphate (1-10 nM; 24 h) induces apoptosis by microtubule depolymerization-induced AKT inactivation and the removal of GSK-3β inhibition in HepG2 cells[2].
Combretastatin A-1 phosphate (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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Combretastatin A-1 phosphate tetrasodium 相关抗体:

Western Blot Analysis[2]

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.
体内研究
(In Vivo)

Combretastatin A-1 phosphate (1-4 mg/kg; i.v. every other day for 4 weeks) significantly reduces the tumor volume in HepG2 subcutaneous xenograft model[2].
Combretastatin A-1 phosphate (2 mg/kg; every other day for 21 days) shows enhanced apoptosis in orthotopic hepatocellular carcinoma mouse model[2].

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 cells[2]
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.
分子量

580.23

Formula

C18H18Na4O12P2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Combretastatin A-1 phosphate tetrasodium 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Combretastatin A-1 phosphate tetrasodium288847-34-7OXi-4503 tetrasodiumMicrotubule/TubulinmicrotubulepolymerizationcolchicinetubulinWntβ-cateninAKTanti-tumoranti-vascularInhibitorinhibitorinhibit

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