Fosbretabulin disodium (Synonyms: CA 4DP; CA 4P; Combretastatin A4 disodium phosphate)

Cat. No.: HY-17449 Purity: 99.47%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

Fosbretabulin disodium Chemical Structure

CAS No. : 168555-66-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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Other Forms of Fosbretabulin disodium:

Fosbretabulin Get quote
Fosbretabulin tromethamine Get quote

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Description

IC₅₀ & Target

tubulin^[1]

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]

In Vitro

Fosbretabulin disodium inhibits growth of leukemia P-388, pancreas BXPC-3,?neuroblast SK-N-SH, thyroid SW1736, lung-NSC NCI-H460, prostate DU-145, an pharynx FADU, with EC₅₀s of 0.0029, 0.23, 0.00025, 0.00061, 0.00035, 0.00072, and 0.00045 μg/mL, respectively^[2].

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

In Vivo

Fosbretabulin disodium (100 mg/kg; i.p.) increases the mean arterial blood pressure (MABP) at 1 and 6 h after administration and decreases the tumor blood flow in rats^[3].

MedChemExpress (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

Molecular Weight

440.29

Formula

C₁₈H₁₉Na₂O₈P

CAS No.

168555-66-6

Appearance

Solid

Color

White to off-white

SMILES

COC1=C(OC)C(OC)=CC(/C=C\C2=CC=C(OC)C(OP(O[Na])(O[Na])=O)=C2)=C1

Structure Classification

Stilbenes

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

H₂O : 4.5 mg/mL (10.22 mM; Need ultrasonic and warming)

DMF : < 1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.2271 mL	1.1356 mL	2.2712 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 14.29 mg/mL (32.46 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Calculation results:

Working solution concentration: mg/mL

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.47%

Select Batch:

Data Sheet (286 KB) SDS (393 KB)

COA (265 KB) HNMR (165 KB) LCMS (394 KB)

Handling Instructions (2659 KB)

References

[1]. Shen CH, et, al. Combretastatin A-4 inhibits cell growth and metastasis in bladder cancer cells and retards tumour growth in a murine orthotopic bladder tumour model. Br J Pharmacol. 2010 Aug;160(8):2008-27. [Content Brief]

[2]. Pettit GR, et, al. Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41. J Med Chem. 2005 Jun 16;48(12):4087-99. [Content Brief]

[3]. Tozer GM, et, al. Combretastatin A-4 phosphate as a tumor vascular-targeting agent: early effects in tumors and normal tissues. Cancer Res. 1999 Apr 1;59(7):1626-34. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Fosbretabulin disodium Related Classifications

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.

Keywords:

Fosbretabulin disodium168555-66-6CA 4DP CA 4PCombretastatin A4 disodiumMicrotubule/TubulinApoptosistubulindestabilizingendothelianascenttumourneovesselsInhibitorinhibitorinhibit

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Fosbretabulin disodium (Synonyms: CA 4DP; CA 4P; Combretastatin A4 disodium phosphate)

Other Forms of Fosbretabulin disodium:

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