• All
  • Primary Antibodies
  • Conjugated Antibodies for IF
  • Conjugated Antibodies for FC
  • Secondary Antibodies
  • Antibody Labeling KitsNew
  • ELISA Kits
  • IHC Kits
  • Magnetic Cell Separation Kits
  • Cytokines & Growth Factors
  • Neutralizing/activating Antibodies
  • Nanobody-based Reagents
  • Accessory Products and Kits
  • Fusion Proteins
×
×
Host
0
Species Reactivity
0
Species Reactivity
0
Conjugate
0
Conjugate
0
Compatible Species
0
Conjugate
0

Fosbretabulin Disodium

CAS号

168555-66-6

分子式

C18H19O8P·2Na

主要靶点

Apoptosis|Microtubule Associated

仅限科研使用

Cat No : CM05127

Print datasheet

Synonyms

destabilizing|endothelia|Fosbretabulin|Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium|Fosbretabulin Disodium|Apoptosis|Combretastatin A4 disodium|Combretastatin A4 disodium phosphate|Combretastatin A4 disodium Phosphate|Combretastatin A4 Phosphate|CA 4DP|CA 4P|Microtubule/Tubulin|Microtubule Associated|MicrotubuleAssociated|inhibit|Inhibitor|nascent|neovessels|福他布林|tubulin|Tubulin|tumour

验证数据展示

  • CAS No.: 168555-66-6

    Fosbretabulin Disodium
    CAS#: 168555-66-6

产品信息

CAS号 168555-66-6
分子式 C18H19O8P·2Na
主要靶点 Apoptosis|Microtubule Associated
主要通路 凋亡|细胞骨架
分子量 440.29
纯度 99.96%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 destabilizing|endothelia|Fosbretabulin|Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium|Fosbretabulin Disodium|Apoptosis|Combretastatin A4 disodium|Combretastatin A4 disodium phosphate|Combretastatin A4 disodium Phosphate|Combretastatin A4 Phosphate|CA 4DP|CA 4P|Microtubule/Tubulin|Microtubule Associated|MicrotubuleAssociated|inhibit|Inhibitor|nascent|neovessels|福他布林|tubulin|Tubulin|tumour

靶点活性

Tubulin:2.4 μM

体内活性

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]

体外活性

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]

溶解度

DMSO:Insoluble;H2O:10 mM

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)

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.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
=
×
×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2