Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.
In Vitro Activity
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. 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. The viability of both EL4 cells and L1210 cells incubated with deferasirox decrease in a concentration-dependent manner.
In Vivo Activity
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.
Storage & Handling
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.
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