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Fosbretabulin Disodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fosbretabulin Disodium图片
CAS NO:168555-66-6
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议

产品名称
Combretastatin A4 Phosphate
CA 4P
福他布林
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium
CA 4DP
Combretastatin A4 disodium phosphate
产品介绍
Fosbretabulin disodium 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。

产品描述

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium, a water-soluble prodrug of Combretastatin A4 (CA4), is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). Fosbretabulin Disodium inhibits the polymerization of tubulin (IC50: 2.4 μM), and also disrupts tumor vasculature.

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]

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]

激酶实验

Tubulin assembly-disassembly: The assembly of microtubules from isolated tubulin is carried out spectrophotometrically at 350 nm and utilises the increase in turbidity which is associated with microtubule formation. Assembly is initiated by temperature increase from 10 to 35 °C. The effect of drugs on the increase in light absorption is carried. Drugs are dissolved in DMSO (<4%), which does not affect control assembly

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)

Cas No.

168555-66-6

分子式

C18H19Na2O8P

分子量

440.295

别名

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

储存和溶解度

H2O:10 mM
DMSO:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years