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

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

Combretastatin A-1 phosphate (OXi-4503) 是 Combretastatin A-1 的前药,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。

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

Combretastatin A-1 phosphate tetrasodium Chemical Structure

CAS No. : 288847-34-7

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生物活性

Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd 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

288847-34-7

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.

参考文献
  • [1]. Stratford MRL, et, al. Quantitative determination of the anticancer prodrug combretastatin A1 phosphate (OXi4503, CA1P), the active CA1 and its glucuronide metabolites in human urine and of CA1 in plasma by HPLC with mass spectrometric detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Jun 1;898:1-6.

    [2]. Mao J, et, al. Combretastatin A-1 phosphate, a microtubule inhibitor, acts on both hepatocellular carcinoma cells and tumor-associated macrophages by inhibiting the Wnt/β-catenin pathway. Cancer Lett. 2016 Sep 28;380(1):134-43.

    [3]. Holwell SE, et, al. Anti-tumor and anti-vascular effects of the novel tubulin-binding agent combretastatin A-1 phosphate. Anticancer Res. Nov-Dec 2002;22(6C):3933-40.

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