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地拉罗司 /Deferasirox {[allProObj[0].p_purity_real_show]}

货号:A340437 同义名: ICL 670;ICL670A

Deferasirox is an oral iron chelator mainly used to reduce chronic iron overload in patients.

Deferasirox 化学结构 CAS号:201530-41-8
Deferasirox 化学结构
CAS号:201530-41-8
Deferasirox 3D分子结构
CAS号:201530-41-8
Deferasirox 化学结构 CAS号:201530-41-8
Deferasirox 3D分子结构 CAS号:201530-41-8
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Deferasirox 生物活性

描述 Deferasirox (ICL 670) is an orally administered iron chelator designed to manage transfusional iron overload[1].[2].[3].
体内研究

Tumors in SIO mice treated with deferasirox are significantly smaller compared to controls, and mice receiving DFX exhibit extended survival. Deferasirox offers a survival advantage in the SIO leukemia murine model, attributed to its iron chelation and anti-leukemic properties[3].

体外研究

In LX-2 cells subjected to 50 μM deferasirox for 12 hours, there's a 25% reduction in α1(I)procollagen expression, with the most significant decreases (up to 10-fold) observed after 24-120 hours of treatment. Additionally, expression of α-smooth muscle actin (αSMA) is notably reduced[1].

Deferasirox demonstrates anti-proliferative effects on HL-60 or KG-1 myeloid leukemia cell lines at concentrations as low as 5 μM, with cytotoxicity being both dose and time-dependent[2].

The viability of EL4 and L1210 cells declines in a concentration-dependent manner when incubated with deferasirox[3].

Deferasirox 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01441375 - Completed - United States, Louisiana ... 展开 >> Tulane University New Orleans, Louisiana, United States, 70112 United States, Tennessee Universit of Tennessee Memphis, Tennessee, United States, 38163 收起 <<
NCT01838291 - Completed - Cyprus ... 展开 >> Thalassemia Center of North Cyprus Turkish Republic (KKTC) Nicosia, Cyprus Egypt Hematology Unit, El-Shatby Children Hospital, Alexandria University Alexandria, Egypt Hematology Unit, Assiut University Hospital Assiut, Egypt Ain Shams University Cairo, Egypt Hematology Unit, Mansoura University Children Hospital Mansoura, Egypt Tanta University Hospital Tanta, Egypt Hematology/Oncology Unit ; Zagazig University Children Hospital Zagazig, Egypt Zagazig University; Thalassemia Association Zagazig, Egypt Oman Department of Child Health, College of Medicine and Health Sciences, Sultan Qaboos University Hospital Muscat, Oman Saudi Arabia King Abdulaziz University Hospital (KAAUH) Jeddah, Saudi Arabia Maternity and Children's Hospital Maddinah, Saudi Arabia Turkey Çukurova Üniversitesi Tip Fakültesi, Çocuk Hematolojie Bilim Dali Adana, Turkey Akdeniz Üniversitesi Hastanesi, Çocuk Sağliği, Hematolojie Kliniği Antalya, Turkey Ïstanbul Üniversitesi Tip. Fak. Hastanesi, Çocuk Sağliği, Hematolojie Kliniği Istanbul, Turkey 收起 <<
NCT01795794 CDA Type I Phase 4 Unknown December 2013 -

Deferasirox 参考文献

[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.

Deferasirox 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.68mL

0.54mL

0.27mL

13.39mL

2.68mL

1.34mL

26.78mL

5.36mL

2.68mL

Deferasirox 技术信息

CAS号201530-41-8
分子式C21H15N3O4
分子量 373.361
别名 ICL 670;ICL670A;Desifer.;Defrijet;Desirox;Deferasirox. Brand name: Exjade;CGP-72670
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Inert atmosphere,2-8°C

溶解方案

DMSO: 105 mg/mL(281.23 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方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,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方

5% DMSO+40% PEG 300+5%Tween 80 +50 % water 3.7 mg/mL

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