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

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Chemical Structure

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。

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客户使用Selleck生产的Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium发表文献10篇：

客户使用该产品的3个实验数据：

  • 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.

  • 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。
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
Tubulin [1]
(Cell-free assay)
2.4 μM
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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV3 cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 M2fJUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vPWlMh[2WubIOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygTWM2OD1yLkCwOFUh|ryP MnzFNlA6PzN2OEi=
HeLa cells NYDYOm52WHKxbHnm[ZJifGmxbjDhd5NigQ>? NF7UTZJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygTWM2OD1yLkCwOFch|ryP M3O3XlIxQTd|NEi4
rat A10 cells MmTXSpVv[3Srb36gZZN{[Xl? MXzJcohq[mm2aX;uJI9nKG2rY4LveJVjfWynIHTldI9tgW2ncnn6ZZRqd25iaX6gdoF1KEFzMDDj[YxteyCjc4Pld5Nm\CCjczDy[Y9z\2GwaYrheIlwdiCxZjDpcpRmenCqYYPlJI1q[3KxdIXieYxmKG6ndIfvdosh[nliaX7kbZJm[3RiaX3teY5w\my3b4Lld4NmdmOnIITlZ4hvcXG3ZTygSWM2OD1yLkCwO{DPxE1? M1z1RlIxQTd|NEi4

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Immunofluorescence
tubulin / VE-cadherin; 

PubMed: 29221156     


HUVEC monolayers were treated with 1 μM CA4P for 4 (A, E), 8 (B, F), or 10 (C, G) minutes then fixed and stained for either tubulin (A-D) or VE-cadherin (E-H). HUVEC were also pretreated with 1 μM S1P prior to CA4P treatment; (D,H) show tubulin and VE-cadherin staining following S1P pretreatment followed by 10 minutes CA4P treatment. Tubulin disruption and VE-cadherin rearrangement are both evident from around 8 minutes post CA4P treatment (arrowheads). Tubulin disruption is pronounced by 10 minutes after starting CA4P treatment (*) but tubulin is protected at this timepoint by pretreatment with S1P (**). Scale bars = 5μm.

Actin / N-cadherin / CD31 ; 

PubMed: 29221156     


Untreated co-cultured HUVEC and vSMC stained for CD31 (indicating endothelial cells) and N-cadherin (indicating EC/SMC junctions) display mostly intact CD31 and N-cadherin staining at intercellular junctions (A, C, E), although some cytoplasmic N-cadherin is also evident. Staining for F-actin in (A) and (B), indicated in red, reveals the cytoskeleton of the cells. (A) shows untreated co-cultures in monolayer stained for N-cadherin (green) and actin (red), whilst (B) shows CA4P treated cells. (C) shows a tubular structure, typically formed from around 40% of the co-cultured cells, with the rest forming flat monolayers as in (E); N-cadherin (red) and CD31 (green). CD31 staining was relatively unaffected by CA4P treatment (green staining in (D) and (F) versus (C) and (E)). However, N-cadherin staining appears considerably more intracellular and punctate following CA4P treatment (green staining in (B) versus (A) and red staining in (F) versus (E). The change in cellular distribution of N-cadherin following CA4P treatment was blocked by pre-treatment with 1μM S1P, allowing N-cadherin to retain its intercellular location, although its appearance was less smooth than in untreated cells (red staining in (G)versus (F)). Cells treated with S1P alone also retained intercellular location of N-cadherin, but with a less smooth appearance than in untreated cells (red staining in (H) versus (E)). Yellow in merged images indicates co-localisation at cell-cell junctions. Arrowheads = EC, asterisks = SMC (revealed by lack of CD31 staining). Scalebars = 15μm.

29221156
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：

[1]
- 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。
细胞实验：

[4]
- 合并
  • Cell lines: HUVECs
  • Concentrations: ~50 nM
  • Incubation Time: 12-48小时
  • Method:

    增殖实验中，FBS在X-VIVO培养基中稀释到最低浓度（1%），以便使内皮细胞有足够的生存能力。分离后，细胞按2×104HUVECs浓度接种到24孔板中，粘附过夜，在有或无细胞因子(5 ng/ml FGF-2 或 5 ng/ml VEGF-A)的情况下继续培养。添加0-50 nMCA4P。温育12，24，36，和48小时后，使用胰蛋白酶/ EDTA分离细胞，通过台酚蓝染色排除法进行手工计数。


    (Only for Reference)
动物实验：

[5]
- 合并
  • Animal Models: 含移植瘤的BD9大鼠
  • Dosages: 100 mg/kg, 3 ml/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 Water 28 mg/mL (63.59 mM)
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
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

计算器

摩尔浓度计算器

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

  • 质量
    浓度
    体积
    分子量

*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

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 )

  • C1
    V1
    C2
    V2

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。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID