Deferasirox

Names

[ CAS No. ]:
201530-41-8

[ Name ]:
Deferasirox

[Synonym ]:
ICL-670
Exjade
Deferasirox

Biological Activity

[Description]:

Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Others

[In Vitro]

In LX-2 cells treated with 50 μM deferasirox for 12 h, α1(I)procollagen expression is decreased by 25%, with maximal reductions (10-fold) seen following 24-120 h of treatment. Similarly, α-smooth muscle actin (αSMA) expression is significantly lower[1]. Deferasirox had anti-proliferative effects on HL-60 or KG-1 myeloid leukemia cell lines at a concentration as low as 5 μM . The cytotoxicity is both dose and time dependent[2]. The viability of both EL4 cells and L1210 cells incubated with deferasirox decrease in a concentration-dependent manner[3].

[In Vivo]

The tumor is significantly smaller in the SIO mice treated with deferasirox compared with control. Mice treated with DFX showed longer survival than the other groups. Deferasirox has a survival benefit for SIO leukemia murine model in terms of iron chelation and antileukemic therapy[3].

[Cell Assay]

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 admin]

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].

[References]

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
672.1±65.0 °C at 760 mmHg

[ Melting Point ]:
260-262ºC

[ Molecular Formula ]:
C₂₁H₁₅N₃O₄

[ Molecular Weight ]:
373.362

[ Flash Point ]:
360.3±34.3 °C

[ Exact Mass ]:
373.106262

[ PSA ]:
107.95000

[ LogP ]:
6.43

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.699

[ Storage condition ]:
-20°C Freezer

Safety Information

[ Hazard Codes ]:
Xi

[ HS Code ]:
2933990090

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%