福他布林|T6272

Fosbretabulin Disodium
168555-66-6

￥282 1mg 起订

￥397 2mg 起订

￥675 5mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 福他布林

英文名称：: Fosbretabulin Disodium

CAS号：: 168555-66-6

品牌：: TargetMol

产地：: 美国

保存条件：: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.96%

产品类别：: 抑制剂

货号：: T6272

Product Introduction

Bioactivity

Name	Fosbretabulin Disodium
Description	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.
Cell Research	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)
Kinase Assay	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
In vitro	Fosbretabulin disodium（Combretastatin A-4 phosphate disodium, CA4P disodium）是可溶于水的前药，源自非洲树木Combretum caffrum的combretastatin A4（CA4）。CA4作为一种结合微管蛋白的剂量，在β-微管蛋白的秋水仙素结合位点或其附近结合（Kd = 0.40 μM），以IC50为2.4 μM抑制微管蛋白组装。[1] CA4对增殖中而非静止的内皮细胞具有细胞毒性，对肿瘤血管具有强大且选择性的毒性。[2] CA4P（1 mM, 30分钟）破坏了内皮细胞的微管骨架并影响其形态，通过Rho/Rho激酶路径引发细胞形态改变，促进肌动蛋白应力纤维的形成及膜泡化，增加细胞层的渗透性。[3] CA4P通过打断VE-cadherin/β-catenin/Akt信号路径主要抑制内皮细胞的迁移和毛细血管管形成，从而增加内皮细胞的渗透性，并导致快速的血管崩溃和肿瘤坏死。[4]
In vivo	CA4P在实验性肿瘤模型中，通过单次给药，剂量为最大耐受剂量(MTD)的10%，可迅速、广泛且不可逆地导致血管关闭。CA4P在化合物给药后6小时内，可使血管体积减少93%。[2] CA4P（100 mg/kg，给药后6小时）使肿瘤血流量大约减少了100倍，而脾脏的血流量大约减少了7倍。[5]
Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	H2O : 10 mM DMSO : Insoluble
Keywords	Microtubule/Tubulin \| tumour \| endothelia \| Apoptosis \| tubulin \| Combretastatin A4 disodium Phosphate \| Combretastatin A4 disodium \| inhibit \| Fosbretabulin Disodium \| neovessels \| destabilizing \| Inhibitor \| Fosbretabulin \| nascent
Inhibitors Related	Meclizine dihydrochloride \| Oleic acid \| Metronidazole \| 5-Fluorouracil \| Dextran sulfate sodium salt (MW 4500-5500) \| Stavudine \| Tributyrin \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Salicylic acid \| Sodium 4-phenylbutyrate
Related Compound Libraries	Anti-Cancer Active Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Selected Plant-Sourced Compound Library \| Natural Product Library \| Microtubule-Targeted Compound Library \| Anti-Cancer Clinical Compound Library

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

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子