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> Fosbretabulin (disodium) [168555-66-6]

Fosbretabulin (disodium) [168555-66-6]

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Référence HY-17449-5mg

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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.

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Fosbretabulin disodium Chemical Structure

Fosbretabulin disodium Chemical Structure

CAS No. : 168555-66-6

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Description

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]
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.

Fosbretabulin disodium Related Antibodies
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.
Essai clinique
Masse moléculaire

440.29

Formule

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
  • Plants
  • other families
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

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

Solvant et solubilité
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
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.

  • Calculateur de molarité

  • Calculateur de dilution

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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).
Pureté et documentation
Références

  • [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]

  • [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.

    [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.

    [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.

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.

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.

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Fosbretabulin disodium Related Classifications

  • Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  • Microtubule/Tubulin Apoptosis
Help & FAQs

Keywords:

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

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