Deferasirox

An iron chelator with anticancer activity

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2mg

￥375.00

300.00

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5mg

￥637.00

510.00

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10mg

￥1150.00

920.00

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25mg

￥2450.00

1960.00

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50mg

￥4112.00

3290.00

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100mg

￥6625.00

5300.00

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Background

Deferasirox is an iron chelator [1].

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 [1].

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 [1]. In two oesophageal adenocarcinoma cell lines OE33 and OE19, deferasirox with a standard chemotherapeutic agent inhibited cellular viability and proliferation [2].

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 [1]. In human xenograft models, deferasirox significantly inhibited tumour growth, which was associated with the decrease in iron levels [2].

参考文献:
[1].? 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.
[2].? 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.

Protocol

Cell experiment:

Deferasirox is dissolved in DMSO. HL-60 or KG-1 cells are treated with 0, 5, 10, 50 μM of deferasirox for 24 or 48 h, and proliferation is determined by an MTT assay[2].

Animal experiment:

Mice: Murine leukemia cells are injected subcutaneously into the right flank of mice. Deferasirox is dissolved in distilled water and orally administered at 20 mg/kg until the cumulative dose reaches 300 mg/kg. The mice are observed and weighed daily[3].

参考文献:

[1]. Sobbe A, et al. Inconsistent hepatic antifibrotic effects with the iron chelator deferasirox. J Gastroenterol Hepatol. 2015 Mar;30(3):638-45.
[2]. Kim JL, et al. The oral iron chelator deferasirox induces apoptosis in myeloid leukemia cells by targetingcaspase. Acta Haematol. 2011;126(4):241-5.
[3]. Lee DH, et al. Deferasirox shows in vitro and in vivo antileukemic effects on murine leukemic cell lines regardless of iron status. Exp Hematol. 2013 Jun;41(6):539-46.