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Fosbretabulin Disodium

Fosbretabulin Disodium (CA 4P) 是一种微管蛋白去稳定剂，是 Combretastatin A4 前药，可选择性靶向内皮细胞，诱导新生肿瘤新血管消退，减少肿瘤血流量并引起中央肿瘤坏死。

CAS号

168555-66-6

分子式

C18H19O8P·2Na

主要靶点

Apoptosis|Microtubule Associated

仅限科研使用

Cat No : CM05127

Print datasheet

Synonyms

CA 4DP|Combretastatin A4 Phosphate|Combretastatin A4 disodium phosphate|福他布林|CA 4P|Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

验证数据展示

  • CAS No.: 168555-66-6

    Fosbretabulin Disodium
    CAS#: 168555-66-6

产品信息

Fosbretabulin Disodium (CA 4P), a water-soluble prodrug of Combretastatin A4 (CA4), is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). Fosbretabulin Disodium(Combretastatin A4 disodium phosphate) inhibits the polymerization of tubulin (IC50: 2.4 μM), and also disrupts tumor vasculature.

CAS号 168555-66-6
分子式 C18H19O8P·2Na
主要靶点 Apoptosis|Microtubule Associated
主要通路 凋亡|细胞骨架
分子量 440.29
纯度 99.83%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 CA 4DP|Combretastatin A4 Phosphate|Combretastatin A4 disodium phosphate|福他布林|CA 4P|Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

靶点活性

Tubulin:2.4 μM

体内活性

CA4P causes rapid, extensive and irreversible vascular shutdown in experimental tumor models following the administration of a single dose at 10% of the maximum tolerated dose (MTD). CA4P causes a 93% reduction in vascular volume 6 h following drug administration. [2] CA4P(100 mg/kg, 6 h following administration) reduces tumor blood by approximately 100-fold, compared with approximately 7-fold in the spleen. [5]

体外活性

Fosbretabulin disodium (Combretastatin A-4 phosphate disodium, CA4P disodium) is the water-soluble prodrug of combretastatin A4 (CA4), which is originally isolated from African tree Combretum caffrum. CA4 is a tubulin-binding agent that binds at or near the colchicine binding site of β-tubulin (Kd = 0.40 μM), inhibits tubulin assembly with IC50 of 2.4 μM. [1] CA4 is cytotoxic towards proliferating but not quiescent endothelial cells, has potent and selective toxicity towards tumor vasculature. [2] CA4P (1 mM, 30 minutes) disrupts the endothelial microtubule cytoskeleton and mediates changes in endothelial cell morphology. CA4P stimulates actin stress fiber formation and membrane blebbing and increases monolayer permeability via Rho/Rho-kinase. [3] CA4P increases endothelial cell permeability, while inhibiting endothelial cell migration and capillary tube formation predominantly through disruption of VE-cadherin/β-catenin/Akt signaling pathway, thereby leading to rapid vascular collapse and tumor necrosis. [4]

溶解度

DMSO:Insoluble,H2O:10 mM

细胞实验

For the proliferation assay, the minimal concentration of FBS (1%) diluted in X-VIVO medium is used to allow sufficient viability of endothelial cells. After detachment, the cells are seeded at a concentration of 2×104 HUVECs in each well of 24-well plates, allowed to adhere overnight, and then incubated with or without cytokines (5 ng/ml FGF-2 or 5 ng/ml VEGF-A). CA4P is added at 0 – 50 nM. After incubation for 12, 24, 36, and 48 hours, cells are detached by trypsin/EDTA and manually counted using trypan blue exclusion. (Only for Reference)

参考文献

1.Woods JA, et al. Br J Cancer 1995, 71(4), 705-711.
2.Dark GG, et al. Cancer Res 1997, 57(10), 1829-1834.
3.Kathou C, et al. Blood, 2002, 99(6), 2060-2069.
4.Vincent L, et al. J Clin Invest, 2005, 115(11), 21992-32006.
5.Tozer GM, et al. Cancer Res, 1999, 59(7), 1626-1634.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2