Deferasirox is an iron chelator .
Iron chelate is a soluble complex of iron, sodium and a chelating agent and used to make the iron soluble in water. Iron chelators were initially developed for the treatment of iron overload for clinical use .
Deferasirox is an orally iron chelator used for the treatment of iron-overload disease. In DMS-53 lung carcinoma and SK-N-MC neuroepithelioma cell lines, deferasirox inhibited cells proliferation. Deferasirox inhibited iron uptake from human transferrin and mobilized cellular 59Fe . In two oesophageal adenocarcinoma cell lines OE33 and OE19, deferasirox with a standard chemotherapeutic agent inhibited cellular viability and proliferation .
In nude mice bearing DMS-53 lung carcinoma xenografts, deferasirox inhibited tumor growth. Also, deferasirox increased cleaved caspase-3, cleaved poly(ADP-ribose) polymerase 1, the cyclin-dependent kinase inhibitor p21CIP1/WAF1 and the expression of the metastasis suppressor protein N-myc downstream-regulated gene 1 while reducing cyclin D1, which suggested deferasirox is an effective antitumor agent . In human xenograft models, deferasirox significantly inhibited tumour growth, which was associated with the decrease in iron levels .
. Lui GY, Obeidy P, Ford SJ, et al. The iron chelator, deferasirox, as a novel strategy for cancer treatment: oral activity against human lung tumor xenografts and molecular mechanism of action. Mol Pharmacol, 2013, 83(1): 179-190.
. Ford SJ, Obeidy P, Lovejoy DB, et al. Deferasirox (ICL670A) effectively inhibits oesophageal cancer growth in vitro and in vivo. Br J Pharmacol, 2013, 168(6): 1316-1328.
|Storage||Store at -20°C|
|Solubility||≥11.9mg/mL in DMSO|
|Chemical Name||4-(3,5-bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl)benzoic acid|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|