福他布林 T6272

Product Introduction
Bioactivity


英文名: Fosbretabulin Disodium

描述: 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。

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)

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

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]

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 10 mM
DMSO : Insoluble


关键字: Microtubule/Tubulin | tumour | endothelia | Apoptosis | tubulin | Combretastatin A4 disodium Phosphate | Combretastatin A4 disodium | inhibit | Fosbretabulin Disodium | neovessels | destabilizing | Inhibitor | Fosbretabulin | nascent

相关产品: BQZ-485 | GSK1324726A | PU02 | Glycochenodeoxycholic Acid | D-Mannitol | MKC-1 | Alofanib | Palomid 529 | Ligustrazine | Didymin

相关库: Drug Repurposing Compound Library | Approved Drug Library | ReFRAME Related Library | Microtubule-Targeted Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | Preclinical Compound Library

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