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Fosbretabulin Disodium

产品编号 T6272 CAS 168555-66-6

别名: Combretastatin A4 Phosphate, CA 4DP, CA 4P, 福他布林, Combretastatin A4 disodium phosphate, Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) 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。

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Fosbretabulin Disodium Chemical Structure

Fosbretabulin Disodium, CAS 168555-66-6

规格	价格/CNY	货期
1 mg	￥ 282	现货
2 mg	￥ 397	现货
5 mg	￥ 675	现货
10 mg	￥ 990	现货
25 mg	￥ 1,780	现货
50 mg	￥ 2,730	现货
100 mg	￥ 3,990	现货

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其他形式的 Fosbretabulin Disodium:

Fosbretabulin [free base]
询价

选择批次

纯度: 99.96%

纯度: 99.83%

纯度: 97.43%

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天然产物信息

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

植物来源	天然产物 > 其他（植物来源） > 其他

产品描述	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.
靶点活性	Tubulin:2.4 μM
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)

别名	Combretastatin A4 Phosphate, CA 4DP, CA 4P, 福他布林, Combretastatin A4 disodium phosphate, Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium
分子量	440.29
分子式	C18H19O8P·2Na
CAS No.	168555-66-6

存储

store at low temperature　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 10 mM

DMSO: Insoluble

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
H2O	1 mM	2.2712 mL	11.3562 mL	22.7123 mL	56.7808 mL
	5 mM	0.4542 mL	2.2712 mL	4.5425 mL	11.3562 mL
	10 mM	0.2271 mL	1.1356 mL	2.2712 mL	5.6781 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

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.

文献引用

1. Han T, Duan Q, Yang R, et al. Monitoring the therapeutic efficacy of CA4P in the rabbit VX2 liver tumor using dynamic contrast-enhanced MRI. Diagnostic and Interventional Radiology. 2021, 27(5): 587. 2. Meng F, Zou B, Yang R, et al. The diagnostic efficiency of the perfusion-related parameters in assessing the vascular disrupting agent (CA4P) response in a rabbit VX2 liver tumor model. Acta Radiologica. 2021: 02841851211032450.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Fosbretabulin Disodium 168555-66-6 Apoptosis Cytoskeletal Signaling Microtubule Associated Microtubule/Tubulin Combretastatin A4 Phosphate tumour endothelia CA 4DP CA 4P 福他布林 Combretastatin A4 disodium phosphate tubulin Combretastatin A4 disodium Phosphate Combretastatin A4 disodium inhibit Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium neovessels destabilizing Inhibitor Fosbretabulin nascent inhibitor

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Fosbretabulin Disodium

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords