Cas No.: | 201530-41-8 |
Synonyms: | Exjade, ICL-670, ICL-670A, CGP-72670 |
SMILES: | O=C(O)C1=CC=C(N2N=C(C3=CC=CC=C3O)N=C2C4=CC=CC=C4O)C=C1 |
Formula: | C21H15N3O4 |
M.Wt: | 373.36 |
Purity: | >99% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload. |
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]. |
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]. |
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 Administration: | 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. |