1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin

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

Cat. No.: HY-17449 Purity: 99.73%
Data Sheet SDS Handling Instructions

Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.

For research use only. We do not sell to patients.
Fosbretabulin disodium Chemical Structure

Fosbretabulin disodium Chemical Structure

CAS No. : 168555-66-6

Size Price Stock Quantity
10 mM * 1 mL in Water $106 In-stock
5 mg $96 In-stock
10 mg $120 In-stock
50 mg $350 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis. IC50 Value: 4 nM [1] Target: microtubule in vitro: Cytotoxic IC(50) values of CA-4 in human bladder cancer cells were below 4 nM. Analyses of cell-cycle distribution showed CA-4 obviously induced G(2)-M phase arrest with sub-G(1) formation. The analyses of apoptosis showed that CA-4 induced caspase-3 activation and decreased BubR1 and Bub3 in cancer cells [1]. The enhanced apoptosis induced by dasatinib plus CA-4 was accompanied by a greater extent of mitochondrial depolarization, caspase-3 activation and PARP cleavage in HO-8910 cells. Furthermore, elevated expression of Mcl-1 led to a reduced apoptosis induced by dasatinib plus CA-4, highlighting that downregulated Mcl-1 was necessary for the potentiating effect of dasatinib to CA-4-triggered apoptosis [2]. in vivo: The increased anticancer efficacy of dasatinib combined with CA-4 was further validated in a human HO-8910 ovarian cancer xenograft model in nude mice [2]. There was a significant, concentration dependent increase in mean arterial blood pressure with a maximum increase of about 60% of the baseline MAP at 30 mg/kg of CA4P compared to the saline control. However, there was no significant increase in the cardiac troponin I level after CA4P injection [3]. Clinical trial: A phase II trial of fosbretabulin in advanced anaplastic thyroid carcinoma and correlation of baseline serum-soluble intracellular adhesion molecule-1 with outcome [4].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01305213 National Cancer Institute (NCI) Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma March 2011 Phase 2
NCT02641639 Mateon Therapeutics Platinum Resistant Ovarian Cancer June 2016 Phase 2|Phase 3
NCT02132468 Mateon Therapeutics Neuroendocrine Tumors September 2014 Phase 2
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References
Molecular Weight

440.29

Formula

C₁₈H₁₉Na₂O₈P

CAS No.

168555-66-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

H2O: 4.4 mg/mL (Need ultrasonic and warming); DMSO: < 0.044 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Fosbretabulin disodium
Cat. No.:
HY-17449
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