Deferasirox-ICL-670-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDeferasiroxCat. No.: HY-17359CAS No.: 201530-41-8Synonyms: ICL 670分式: CHNO分量: 373.36作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (267.84 mM)* means solubl

2、e, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.6784 mL 13.3919 mL 26.7838 mL5 mM 0.5357 mL 2.6784 mL 5.3568 mL10 mM 0.2678 mL 1.3392 mL 2.6784 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使

3、；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.70 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.70 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请

4、依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.70 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Deferasirox (ICL 670)具有活性的，于治疗铁离过量的螯合剂。体外研究 In LX-2 cells treated with 50M deferasirox for 12h, 1(I)procollagen expression is decreased by 25%, withmaximal reductions (10-fold) seen following 24-120h

5、 of treatment. Similarly, -smooth muscle actin (SMA)expression is significantly lower 1. Deferasirox had anti-proliferative effects on HL-60 or KG-1 myeloidleukemia cell lines at a concentration as low as 5 M . The cytotoxicity is both dose and time dependent 2.The viability of both EL4 cells and L1

6、210 cells incubated with deferasirox decrease in a concentration-dependent manner 3.体内研究 The tumor is significantly smaller in the SIO mice treated with deferasirox compared with control. Micetreated with DFX showed longer survival than the other groups. Deferasirox has a survival benefit for SIOleu

7、kemia murine model in terms of iron chelation and antileukemic therapy 3.PROTOCOLCell Assay 2 Deferasirox is dissolved in DMSO. HL-60 or KG-1 cells are treated with 0, 5, 10, 50 M of deferasirox for 24or 48 h, and proliferation is determined by an MTT assay 2.MCE has not independently confirmed the

8、accuracy of these methods. They are for reference only.Animal Mice: Murine leukemia cells are injected subcutaneously into the right flank of mice. Deferasirox is dissolvedAdministration 3 in distilled water and orally administered at 20 mg/kg until the cumulative dose reaches 300 mg/kg. The miceare

9、 observed and weighed daily 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. 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

10、 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. ExpHematol. 2013 Jun;41(6):539-46.McePdfHeightCaution: Product has not been fully vali