1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. Fosbretabulin disodium

Fosbretabulin disodium  (Synonyms: 康普瑞汀磷酸二钠; CA 4DP; CA 4P; Combretastatin A4 disodium phosphate)

目录号: HY-17449 纯度: 99.47%
COA 产品使用指南

Fosbretabulin disodium (CA 4DP) 是微管蛋白去稳定剂。Fosbretabulin disodium 是 Combretastatin A4 前体,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。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Fosbretabulin disodium Chemical Structure

Fosbretabulin disodium Chemical Structure

CAS No. : 168555-66-6

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Other Forms of Fosbretabulin disodium:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fosbretabulin disodium (CA 4DP) is a tubulin destabilizing agent. Fosbretabulin disodium is the Combretastatin A4 proagent that selectively targets endothelial cells, induces regression of nascent tumour neovessels, reduces tumour blood flow and causes central tumour necrosis[1][3].

IC50 & Target

tubulin[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 GI50
0.32 μM
Compound: CA-4P; 3
Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay
Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay
[PMID: 30580241]
A-375 IC50
0.0016 μM
Compound: CA4P
Growth inhibition of human A375 cells measured after 48 hrs by MTS assay
Growth inhibition of human A375 cells measured after 48 hrs by MTS assay
[PMID: 27100701]
A549 IC50
0.0234 μM
Compound: CA4P
Growth inhibition of human A549 cells by MTS assay
Growth inhibition of human A549 cells by MTS assay
[PMID: 27100701]
A549 GI50
0.16 μM
Compound: CA-4P; 3
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
[PMID: 30580241]
A549 IC50
0.4 μM
Compound: CA-4P
Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 assay
[PMID: 30108925]
Bel-7402 IC50
0.04 μM
Compound: CA-4p
Antiproliferative activity against human Bel-7402 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human Bel-7402 cells measured after 48 hrs by SRB assay
[PMID: 32113125]
BXPC-3 GI50
0.23 μg/mL
Compound: 1b, CA4P, Fosbretabulin
Growth inhibition of human BxPC3 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human BxPC3 cells after 48 hrs by sulforhodamine B assay
[PMID: 22324723]
BXPC-3 GI50
0.23 μg/mL
Compound: CA4P
Antitumor activity against human BxPC3 cells by sulforhodamine B assay
Antitumor activity against human BxPC3 cells by sulforhodamine B assay
[PMID: 19228038]
Caov-3 cell line IC50
13.11 nM
Compound: CA4P
Antiproliferative activity against human Caov3 cells measured after 96 hrs by Celltiter-Glo assay
Antiproliferative activity against human Caov3 cells measured after 96 hrs by Celltiter-Glo assay
[PMID: 27718473]
CCRF-CEM IC50
0.011 μM
Compound: 7; CA-4P
Antiproliferative activity against human CEM cells measured after 96 hrs by Coulter counter method
Antiproliferative activity against human CEM cells measured after 96 hrs by Coulter counter method
[PMID: 30921759]
CCRF-CEM IC50
0.011 μM
Compound: 4; CA-4P
Antiproliferative activity against human CEM cells after 96 hrs by coulter counting method
Antiproliferative activity against human CEM cells after 96 hrs by coulter counting method
[PMID: 29471122]
CCRF-CEM IC50
95 nM
Compound: CA-4P, combretastatin A4P
Antiproliferative activity against human CEM cells after 96 hrs by Coulter counter method
Antiproliferative activity against human CEM cells after 96 hrs by Coulter counter method
[PMID: 25626146]
DU-145 GI50
0.0007 μg/mL
Compound: CA4P
Antitumor activity against human DU145 cells by sulforhodamine B assay
Antitumor activity against human DU145 cells by sulforhodamine B assay
[PMID: 19228038]
DU-145 IC50
0.0014 μM
Compound: CA4P
Growth inhibition of human DU145 cells measured after 48 hrs by MTS assay
Growth inhibition of human DU145 cells measured after 48 hrs by MTS assay
[PMID: 27100701]
DU-145 GI50
0.00323 μM
Compound: CA-4P
Cytotoxicity against human DU145 cells assessed as growth inhibition measured after 48 hrs by SRB assay
Cytotoxicity against human DU145 cells assessed as growth inhibition measured after 48 hrs by SRB assay
[PMID: 31059248]
DU-145 GI50
0.00323 μM
Compound: CA4P
Cytotoxicity against human DU145 cells after 48 hrs by SRB assay
Cytotoxicity against human DU145 cells after 48 hrs by SRB assay
[PMID: 24183586]
DU-145 GI50
0.0072 μg/mL
Compound: 1b, CA4P, Fosbretabulin
Growth inhibition of human DU145 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human DU145 cells after 48 hrs by sulforhodamine B assay
[PMID: 22324723]
DU-145 GI50
0.016 μM
Compound: 3, CA4P
Cytotoxicity against human DU145 cells by SRB assay
Cytotoxicity against human DU145 cells by SRB assay
[PMID: 24016002]
HCT-116 IC50
0.0016 μM
Compound: CA4P
Growth inhibition of human HCT116 cells measured after 48 hrs by MTS assay
Growth inhibition of human HCT116 cells measured after 48 hrs by MTS assay
[PMID: 27100701]
HCT-116 IC50
0.24 μM
Compound: CA-4P
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay
[PMID: 30108925]
HeLa IC50
0.00043 μM
Compound: 2, CA4-P
Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
[PMID: 19879758]
HeLa IC50
0.013 μM
Compound: 7; CA-4P
Antiproliferative activity against human HeLa cells measured after 3 days by Coulter counter method
Antiproliferative activity against human HeLa cells measured after 3 days by Coulter counter method
[PMID: 30921759]
HeLa IC50
0.013 μM
Compound: 4; CA-4P
Antiproliferative activity against human HeLa cells after 3 days by coulter counting method
Antiproliferative activity against human HeLa cells after 3 days by coulter counting method
[PMID: 29471122]
HeLa GI50
0.019 μM
Compound: CA-4P; 3
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 30580241]
HeLa IC50
0.56 μM
Compound: CA-4P
Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay
[PMID: 30108925]
HeLa IC50
79 nM
Compound: CA-4P, combretastatin A4P
Antiproliferative activity against human HeLa cells after 4 days by Coulter counter method
Antiproliferative activity against human HeLa cells after 4 days by Coulter counter method
[PMID: 25626146]
HepG2 IC50
0.002 μM
Compound: CA-4p
Antiproliferative activity against human HepG2 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human HepG2 cells measured after 48 hrs by SRB assay
[PMID: 32113125]
HepG2 GI50
0.19 μM
Compound: CA-4P; 3
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 30580241]
HepG2 IC50
0.27 μM
Compound: CA-4P
Antiproliferative activity against human HepG2 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human HepG2 cells after 72 hrs by CCK-8 assay
[PMID: 30108925]
HMEC-1 IC50
0.0029 μM
Compound: 7; CA-4P
Antiproliferative activity against human HMEC1 cells measured after 4 days by Coulter counter method
Antiproliferative activity against human HMEC1 cells measured after 4 days by Coulter counter method
[PMID: 30921759]
HMEC-1 IC50
0.0029 μM
Compound: 4; CA-4P
Antiproliferative activity against human HMEC1 cells after 4 days by coulter counting method
Antiproliferative activity against human HMEC1 cells after 4 days by coulter counting method
[PMID: 29471122]
HMEC-1 IC50
2.9 nM
Compound: CA-4P, combretastatin A4P
Antiproliferative activity against human HMEC1 cells after 4 days by Coulter counter method
Antiproliferative activity against human HMEC1 cells after 4 days by Coulter counter method
[PMID: 25626146]
HT-29 GI50
0.062 μM
Compound: CA-4P; 3
Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
[PMID: 30580241]
HUVEC GI50
8 nM
Compound: CA4P
Growth inhibition of HUVEC after 72 hrs by crystal violet staining-based assay
Growth inhibition of HUVEC after 72 hrs by crystal violet staining-based assay
[PMID: 27690431]
Jurkat EC50
15 nM
Compound: CA4P, Zybrestat
Cytotoxicity against human Jurkat cells assessed as cell viability after 48 hrs by trypan blue exclusion assay
Cytotoxicity against human Jurkat cells assessed as cell viability after 48 hrs by trypan blue exclusion assay
[PMID: 24387982]
K562 IC50
0.72 μM
Compound: 7
Cytotoxicity against human K562 cells assessed as growth inhibition after 5 days by MTT assay
Cytotoxicity against human K562 cells assessed as growth inhibition after 5 days by MTT assay
[PMID: 28143677]
KM-20L2 GI50
0.034 μg/mL
Compound: 1b, CA4P, Fosbretabulin
Growth inhibition of human KM20L2 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human KM20L2 cells after 48 hrs by sulforhodamine B assay
[PMID: 22324723]
KM-20L2 GI50
0.034 μg/mL
Compound: 1b, CA4P
Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay
[PMID: 16252907]
L1210 IC50
0.0021 μM
Compound: 4; CA-4P
Antiproliferative activity against mouse L1210 cells after 96 hrs by coulter counting method
Antiproliferative activity against mouse L1210 cells after 96 hrs by coulter counting method
[PMID: 29471122]
L1210 IC50
0.013 μM
Compound: 7; CA-4P
Antiproliferative activity against mouse L1210 cells measured after 96 hrs by Coulter counter method
Antiproliferative activity against mouse L1210 cells measured after 96 hrs by Coulter counter method
[PMID: 30921759]
L1210 IC50
82 nM
Compound: CA-4P, combretastatin A4P
Antiproliferative activity against mouse L1210 cells after 48 hrs by Coulter counter method
Antiproliferative activity against mouse L1210 cells after 48 hrs by Coulter counter method
[PMID: 25626146]
MCF7 IC50
0.002 μM
Compound: 2, CA4-P
Cytotoxicity against human MCF7 cells by MTT assay
Cytotoxicity against human MCF7 cells by MTT assay
[PMID: 19879758]
MCF7 IC50
0.011 μM
Compound: CA-4p
Antiproliferative activity against human MCF7 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human MCF7 cells measured after 48 hrs by SRB assay
[PMID: 32113125]
MCF7 IC50
0.96 μM
Compound: CA-4P
Antiproliferative activity against human MCF7 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells after 72 hrs by CCK-8 assay
[PMID: 30108925]
MDA-MB-231 IC50
0.0028 μM
Compound: CA4P
Growth inhibition of human MDA-MB-231 cells measured after 48 hrs by MTS assay
Growth inhibition of human MDA-MB-231 cells measured after 48 hrs by MTS assay
[PMID: 27100701]
MDA-MB-231 GI50
0.065 μM
Compound: CA-4P; 3
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 30580241]
MDA-MB-231 IC50
173.3 nM
Compound: CA4P
Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by Celltiter-Glo assay
Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by Celltiter-Glo assay
[PMID: 27718473]
MDA-MB-435 IC50
8.75 nM
Compound: CA4P
Antiproliferative activity against human MDA-MB-435 cells measured after 96 hrs by Celltiter-Glo assay
Antiproliferative activity against human MDA-MB-435 cells measured after 96 hrs by Celltiter-Glo assay
[PMID: 27718473]
MGC-803 IC50
0.47 μM
Compound: CA-4P
Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay
[PMID: 30108925]
NCI-H460 GI50
0.0004 μg/mL
Compound: CA4P
Antitumor activity against human NCI-H460 cells by sulforhodamine B assay
Antitumor activity against human NCI-H460 cells by sulforhodamine B assay
[PMID: 19228038]
NCI-H460 GI50
0.00194 μM
Compound: CA-4P
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition measured after 48 hrs by SRB assay
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition measured after 48 hrs by SRB assay
[PMID: 31059248]
NCI-H460 GI50
0.00194 μM
Compound: CA4P
Cytotoxicity against human NCI-H460 cells after 48 hrs by SRB assay
Cytotoxicity against human NCI-H460 cells after 48 hrs by SRB assay
[PMID: 24183586]
NCI-H460 GI50
0.029 μg/mL
Compound: 1b, CA4P, Fosbretabulin
Growth inhibition of human NCI-H460 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human NCI-H460 cells after 48 hrs by sulforhodamine B assay
[PMID: 22324723]
NCI-H460 GI50
0.029 μg/mL
Compound: 1b, CA4P
Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay
[PMID: 16252907]
NCI-H460 GI50
0.066 μM
Compound: 3, CA4P
Cytotoxicity against human NCI-H460 cells by SRB assay
Cytotoxicity against human NCI-H460 cells by SRB assay
[PMID: 24016002]
P388 ED50
0.0004 μg/mL
Compound: 1b, CA4P
Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay
[PMID: 16252907]
P388 ED50
0.0004 μg/mL
Compound: 1b, CA4P, Fosbretabulin
Growth inhibition of mouse P388 cells after 48 hrs by Z1 Beckman/Coulter particle counter analysis
Growth inhibition of mouse P388 cells after 48 hrs by Z1 Beckman/Coulter particle counter analysis
[PMID: 22324723]
PBMC IC50
0.17 μM
Compound: CA4P
Growth inhibition of human PBMC cells measured after 48 hrs by MTS assay
Growth inhibition of human PBMC cells measured after 48 hrs by MTS assay
[PMID: 27100701]
PC-3 IC50
0.0062 μM
Compound: CA4P
Growth inhibition of human PC3 cells measured after 48 hrs by MTS assay
Growth inhibition of human PC3 cells measured after 48 hrs by MTS assay
[PMID: 27100701]
SF-268 GI50
0.036 μg/mL
Compound: 1b, CA4P, Fosbretabulin
Growth inhibition of human SF268 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SF268 cells after 48 hrs by sulforhodamine B assay
[PMID: 22324723]
SF-268 GI50
0.036 μg/mL
Compound: 1b, CA4P
Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay
[PMID: 16252907]
SK-OV-3 GI50
0.00119 μM
Compound: CA-4P
Cytotoxicity against human SKOV3 cells assessed as growth inhibition measured after 48 hrs by SRB assay
Cytotoxicity against human SKOV3 cells assessed as growth inhibition measured after 48 hrs by SRB assay
[PMID: 31059248]
SK-OV-3 GI50
0.00119 μM
Compound: CA4P
Cytotoxicity against human SKOV3 cells after 48 hrs by SRB assay
Cytotoxicity against human SKOV3 cells after 48 hrs by SRB assay
[PMID: 24183586]
SK-OV-3 IC50
0.0077 μM
Compound: CA4P
Growth inhibition of human SKOV3 cells measured after 48 hrs by MTS assay
Growth inhibition of human SKOV3 cells measured after 48 hrs by MTS assay
[PMID: 27100701]
TOV112D IC50
30.85 nM
Compound: CA4P
Antiproliferative activity against human TOV112D cells measured after 96 hrs by Celltiter-Glo assay
Antiproliferative activity against human TOV112D cells measured after 96 hrs by Celltiter-Glo assay
[PMID: 27718473]
体外研究
(In Vitro)

FosbretabuLin disodium 抑制白血病 P-388、胰腺 BXPC-3、成神经细胞 SK-N-SH、甲状腺 SW1736、肺-NSC NCI-H460、前列腺 DU-145、咽 FADU 的生长,EC50 分别为 0.0029、0.23、0.00025、0.00061、0.00035、0.00072 和 0.00045 μg/mL[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

FosbretabuLin disodium (100 mg/kg;ip) 在给药后 1 小时和 6 小时增加平均动脉血压 (MABP),并降低大鼠的肿瘤血流量[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BD9 rats (7-9 weeks) bearing the s.c. implanted P22 tumor[3]
Dosage: 100 mg/kg
Administration: A single i.p. injections
Result: Significantly raised the MABP by about 30%, and reduced the heart rate at 1 h after administration.
Reduced the blood flow in the tumor.
Clinical Trial
分子量

440.29

Formula

C18H19Na2O8P

CAS 号
性状

固体

颜色

White to off-white

中文名称

康普瑞汀磷酸二钠

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 4.5 mg/mL (10.22 mM; 超声加热助溶)

DMF 中的溶解度 : < 1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2712 mL 11.3562 mL 22.7123 mL
5 mM 0.4542 mL 2.2712 mL 4.5425 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 14.29 mg/mL (32.46 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.47%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 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

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Fosbretabulin disodium
目录号:
HY-17449
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