Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium
For research use only. Not for use in humans.
目录号:S7204 别名: CA 4DP 中文名称:康普瑞汀磷酸二钠

CAS No. 168555-66-6
Fosbretabulin (Combretastatin A4 Phosphate, CA4P, CA 4DP) Disodium是水溶性的Combretastatin A4 (CA4)前药,CA4靶向作用于microtubule从而与β-微管蛋白结合,无细胞试验中Kd为0.4 μM。Fosbretabulin Disodium抑制微管蛋白聚合,IC50为2.4 μM,也会干扰肿瘤血管。Fosbretabulin disodium 在内皮细胞中可诱导有丝分裂阻滞和凋亡。Phase 3。
客户使用该产品的3个实验数据:
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Real-time hemodynamic changes in the tumor upon administration of CA4P. Panel A shows the MRI anatomical reference of the tumor, followed by sO2 maps of a slice of brain showing the largest cross section of the tumor at time points 0, 1, 4 and 6 h. post CA4P administration. Panel B shows the real-time sO2 changes in the tumor and contralateral brain occurring immediately post CA4P administration over 1 hour in a representative animal. SD is represented by lighter shades on the graph. Panel C shows the real-time sO2 changes in the tumor and contralateral brain occurring immediately post CA4P administration (n = 4). Panel D shows the quantification of hypoxia in tumors using CAIX as a marker at times 0 (n = 3), 1 (n = 4) and 6 h. (n = 3) post CA4P administration. Unpaired t-test showed statistically significant difference in CAIX staining at 1 hour post CA4P administration compared to 0 and 6 hours. ** ‐ P > 0.01. Black dotted circle and Red full circle denote the ROIs drawn at the tumor and contralateral brain respectively to compute the sO2.
Transl Oncol, 2018, 11(5):1251-1258. Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium purchased from Selleck.
Immunofluorescence analysis of the effects of CA4P on NECs using confocal microscopy. The effects of CA4P (100 nM) on tubulin (pseudo-color green) and actin (pseudo-color red) were evaluated in subconfluent and 100% confluent NECs. Nuclei are shown in pseudo-color blue. CA4P (100 nM) disrupted tubulin on both subconfluent and 100% confluent NECs in a time-dependent manner. In subconfluent NECs, cell morphology was gradually changed from a spindle shape to a round shape, and actin reorganization was observed by adding 100 nM CA4P for 3 h. However, CA4P did not affect cell morphology or actin in 100% confluent NECs. Scale bar = 20 μm. (For interpretation of the references to color in this figure legend, the reader is referred to the web version of this article.)
Res Vet Sci, 2017, 112:222-228. Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium purchased from Selleck.
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Representative images of Dylight 488-tomato lectin (pseudo-colored green) and Alexa-fluor 555-CD31 (pseudo-colored red) immuno-stained frozen sections from xenografted canine osteosarcoma tumors in the different treatment groups: control; combretastatin A-4 phosphate (CA4P, 30 mg/kg); VE-cadherin neutralizing antibody (VEC NAb, 40 μg/mouse); combination treatment (30 mg/kg CA4P 21 h after 40 μg VEC NAb); and CA4P (100 mg/kg). The upper half of this figure shows the image of the whole tumor and the lower half shows a magnified image. Tumors were excised 3 h after CA4P treatment or 24 h after VEC NAb treatment. Scale bars represent 1 mm or 100 μm.
Res Vet Sci, 2018, 122:1-6. Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium purchased from Selleck.
产品安全说明书
Microtubule Associated抑制剂选择性比较
生物活性
产品描述 | Fosbretabulin (Combretastatin A4 Phosphate, CA4P, CA 4DP) Disodium是水溶性的Combretastatin A4 (CA4)前药,CA4靶向作用于microtubule从而与β-微管蛋白结合,无细胞试验中Kd为0.4 μM。Fosbretabulin Disodium抑制微管蛋白聚合,IC50为2.4 μM,也会干扰肿瘤血管。Fosbretabulin disodium 在内皮细胞中可诱导有丝分裂阻滞和凋亡。Phase 3。 | ||||||||||||||||||||||||||||||
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特性 | A microtubule associated inhibitor with higher affinity to β-tubulin vs. Colchicine. Best for advanced solid tumors, anaplastic thyroid cancer, & choroidal neovascularization. | ||||||||||||||||||||||||||||||
靶点 |
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体外研究 |
Fosbretabulin disodium (Combretastatin A-4 phosphate disodium, CA4P disodium)是 Combretastatin A4 (CA4)的水溶性前体药物, 靶向作用于microtubule,最初是从非洲树Combretum caffrum中分离得到的。CA4是微管蛋白结合剂,结合或靠近到β-微管蛋白的秋水仙素结合位点(Kd= 0.40 μM),抑制微管蛋白装配,IC50为2.4 μM。[1]CA4对增殖的内皮细胞而非休眠的内皮细胞具有细胞毒性,对肿瘤血管具有强效的,选择性的毒性。[2]CA4P(1 mM,30分钟)破坏内皮细胞微管骨架,并介导内皮细胞的形态变化。CA4P刺激肌动蛋白应力纤维的形成和膜出泡,且通过Rho/ Rho激酶提高单层通透性。[3]CA4P提高内皮细胞通透性,主要通过干VE-cadherin/β-catenin/Akt信号通路,而抑制内皮细胞迁移和毛细管形成,从而导致快速的血管性虚脱和肿瘤坏死。[4] |
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Cell Data |
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Assay |
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体内研究 | CA4P按10%的最大耐受剂量(MTD)单独给药处理实验性肿瘤模型,导致快速的,广泛的,不可逆的血管关闭。CA4P 处理6小时后,血管容积下降93%。[2]CA4P按100 mg/kg剂量处理6小时后,肿瘤血降低约100倍,脾中降低约7倍。[5] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
激酶实验: |
- 合并
微管蛋白装配-拆卸: 从微管分离的微管蛋白的组装在350nm下通过分光光度法进行,且利用浊度增加,这是与微管形成相关。温度从10°C提升到35°C组装开始。药物促进光吸收。药物溶解于DMSO(<4%),从而不影响对照组装。 |
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细胞实验: |
- 合并
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动物实验: |
- 合并
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溶解度 (25°C)
体外 | Water | 28 mg/mL (63.59 mM) |
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DMSO | Insoluble | |
Ethanol | Insoluble | |
体内 |
从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献): Saline with a few drops of 5% Na2CO3 |
30 mg/mL |
* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
分子量 | 440.29 |
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化学式 | C18H19O8P.2Na |
CAS号 | 168555-66-6 |
储存条件 |
粉状 溶于溶剂 |
别名 | CA 4DP |
动物体内配方计算器 (澄清溶液)
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % ddH2O | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量:
注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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NCT02641639 | Terminated | Drug: Fosbretabulin tromethamine|Drug: Placebo | Platinum Resistant Ovarian Cancer | Mateon Therapeutics | June 2016 | Phase 2|Phase 3 |
NCT02055690 | Terminated | Drug: Pazopanib|Drug: Fosbretabulin | Ovarian Neoplasms|Neoplasms Ovarian|Ovarian Cancer | The Christie NHS Foundation Trust|Novartis|Mateon Therapeutics|East and North Hertfordshire NHS Trust | September 2014 | Phase 1|Phase 2 |
NCT01023295 | Completed | Drug: fosbretabulin|Drug: Saline | Polypoidal Choroidal Vasculopathy | Mateon Therapeutics | July 2009 | Phase 2 |
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