地拉罗司作用机制 - Medchemexpress - MCE中国

1、Product Data SheetDeferasiroxCat. No.: HY-17359CAS No.: 201530-41-8分式: CHNO分量: 373.36作靶点: Bacterial; Ferroptosis作通路: Anti-infection; Apoptosis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 soluble, but saturation unknown.SolventMas

2、s1 mg 5 mg 10 mgConcentration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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。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。以下溶解

3、案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶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 solution此案可获得 2.5 mg/mL (6.70 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取

4、 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 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 solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (6.70 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液

5、加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.70 mM); Clear solution此案可获得 2.5 mg/mL (6.70 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL 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

6、 LX-2 cells treated with 50 M deferasirox for 12 h, 1(I)procollagen expression is decreased by 25%, with maximalreductions (10-fold) seen following 24-120 h of treatment. Similarly, -smooth muscle actin (SMA) expression issignificantly lower1. Deferasirox had anti-proliferative effects on HL-60 or K

7、G-1 myeloid leukemia cell lines at aconcentration as low as 5 M . The cytotoxicity is both dose and time dependent2. The viability of both EL4 cells andL1210 cells incubated with deferasirox decrease in a concentration-dependent manner3.体内研究 The tumor is significantly smaller in the SIO mice treated

8、 with deferasirox compared with control. Mice treated withDFX showed longer survival than the other groups. Deferasirox has a survival benefit for SIO leukemia murine model in terms of iron chelation and antileukemic therapy3.PROTOCOLCell Assay 2 Deferasirox is dissolved in DMSO. HL-60 or KG-1 cells

9、 are treated with 0, 5, 10, 50 M of deferasirox for 24 or 48 h,and proliferation is determined by an MTT assay2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Murine leukemia cells are injected subcutaneously into the right flank of mice.

10、Deferasirox is dissolved inAdministration 3 distilled water and orally administered at 20 mg/kg until the cumulative dose reaches 300 mg/kg. The mice areobserved and weighed daily3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 PLoS Negl Tr

11、op Dis. 2019 Aug 20;13(8):e0007681. bioRxiv. 2019 Oct.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Sobbe A, et al. Inconsistent hepatic antifibrotic effects with the iron chelator deferasirox. J Gastroenterol Hepatol. 2015 Mar;30(3):638-45.Page 2 of 3 www.MedChemE

12、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. 2013Jun;41(6):539-46.McePdfHeightCaution: Product has not been