Deferasirox (ICL-670)

For research use only. Not for use in humans.

目录号:S1712 别名: CGP-72670 中文名称:地拉罗司

Deferasirox (ICL-670) Chemical Structure

CAS No. 201530-41-8

Deferasirox (ICL-670, CGP-72670)是一种铁螯合剂,是cytochrome P450 3A4诱导剂,Cytochrome P450 2C8的抑制剂,Cytochrome P450 1A2抑制剂。Deferasirox 引起的铁损耗可促进BclxL下调和细胞死亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1308.35 现货
RMB 567.03 现货
RMB 977.16 现货
RMB 1704.85 现货
RMB 3835.63 现货
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客户使用Selleck生产的Deferasirox (ICL-670)发表文献9篇:

客户使用该产品的1个实验数据:

  • U2OS cells were cultured with FAC for 24 hours, washed, followed by chelation with 2 chelators (DFO, DFX) -/+ lysosomal protease inhibitors (E-64d and PepstatinA) and analyzed as in panel A. DFX: Deferasirox.

    Nature, 2014, 509(7498):105-9.. Deferasirox (ICL-670) purchased from Selleck.

产品安全说明书

P450 (e.g. CYP17)抑制剂选择性比较

生物活性

产品描述 Deferasirox (ICL-670, CGP-72670)是一种铁螯合剂,是cytochrome P450 3A4诱导剂,Cytochrome P450 2C8的抑制剂,Cytochrome P450 1A2抑制剂。Deferasirox 引起的铁损耗可促进BclxL下调和细胞死亡。
体外研究

Deferasirox 有效螯合来自Rhizopus oryzae 的铁离子,在浓度远低于临床上可实现的血清水平时,在体外对28/29的临床分离的Mucorales有作用。[1] Deferasirox 诱导显著抑制NF-κB的活性,并在28/40的外周血样本中诱导它的活性亚单位p65的一个细胞质封存处于非活性形式。[2] Deferasirox 可抑制3种人髓细胞系(K562,U937和HL60),其IC50在17-50 mM。[3] Deferasirox 是cidal在体外抑制A. fumigatus,MIC和MFC分别时25 毫克/升和50 毫克/升。[5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 MYjDfZRwfG:6aXPpeJkh[XO|YYm= NUPBc2tDQTZiaILz MnrWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTUQvF2= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODByNUewPEc,OjByMEW3NFg9N2F-
MIAPaCa2 NFjpNHNEgXSxdH;4bYNqfHliYYPzZZk> NYrF[GtKQTZiaILz NXTZNHB2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUmDUHHDZVIh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zMN88US=> NUK2TWdPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCwNFU4ODhpPkKwNFA2PzB6PD;hQi=>
SK-N-MC NGryeJlVd3irY3n0fUBie3OjeR?= NXL3NZBnXG:6aXPpeJkhcW5iaIXtZY4hW0tvTj3NR{Bk\WyuczDifUBOXFRibXX0bI9lNCCLQ{WwQVIxNjV2zszN NHrGcpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEC0NVY4Oid-MkCwOFE3PzJ:L3G+
Sf9 MVfGeY5kfGmxbjDhd5NigQ>? MnG1NlAhdWmwcx?= MlewTY5pcWKrdHnvckBw\iCqdX3hckBOWlB2IH;2[ZJmgHC{ZYPz[YQhcW5iU3[5JINmdGxibXXtZpJidmVidnXzbYNt\XNiYYPz[ZN{\WRiYYOgeZB1[WunIH;mJHs{UF1vZYP0doFlcW:uLUG3ZoV1[S2GLXfseYN2em:waXTlJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmRiR2PIJI1m[XO3cnXkJIFnfGW{IEKwJI1qdnNiYomgcYVu[nKjbnWgeoV{cWOuZTD0doFve3CxcoSgZZN{[XluIFnDOVA:OzZwNd88US=> M4fHNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUW2NVAyLz5{M{m1OlExOTxxYU6=
SJ-GBM2 NHOyVI5yUFSVIHHzd4F6 MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MnHxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-37 M{nXTJFJXFNiYYPzZZk> NUjQOXR6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz M4jlV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 MUnxTHRUKGG|c3H5 M4faN5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NIHZdlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 NFnwT5hyUFSVIHHzd4F6 Mk\udWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= MlXGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CDK2 / CDK4 / CDK6 / Cyclin A / Cyclin B / Cyclin D1 / Cyclin E / p53 / p27 / p21 ; 

PubMed: 26965928     


Western blot analysis of cell cycle-related molecules showed that deferasirox upregulated p21, p27, and p53 and downregulated cyclin D1, cyclin B, and CDK4

TFR1 / Ferroportin ; 

PubMed: 26965928     


Treatment with deferasirox for 24 h resulted in an increased level of TFR1 and a decreased level of ferroportin

Pro-caspase-3 / Pro-caspase-8 / Pro-caspase-9 / BAX / NDRG1 / c-Myc / p-mTOR ; 

PubMed: 26965928     


Deferasirox also induced apoptosis, upregulated NDRG1, and downregulated p-mTOR and c-myc as assessed by Western blot analysis

26965928
Immunofluorescence
Bax / TOM22 ; 

PubMed: 28139717     


Deferasirox for 24 hours induces Bax translocation to mitochondria, where it forms aggregates, and colocalizes with mitochondrial receptor TOM22 that appears aggregated (arrowhead). Confocal microscopy: Bax in red, TOM22 in green and DAPI in blue. Original magnification x63, detail x100. Images representative of three experiments.

Cytochrome c; 

PubMed: 28139717     


Localization of cytochrome c in tubular cells exposed to 10 μM deferasirox for 6 hours. Note the punctate mitochondrial pattern in control cells and diffuse labeling in deferasirox-exposed cells (arrowheads). Confocal microscopy. Cytochrome c in green and DAPI in blue, original magnification x63. Images representative of three experiments. 

28139717
Growth inhibition assay
Cell viability; 

PubMed: 26965928     


Cell viability was measured by the MTT assay. AGS, MKN-28, SNU-484, and SNU-638 cells were incubated with 0, 1, 10, 50, and 100 μM of deferasirox at 37 °C for 24, 48, or 72 h. Deferasirox treatment resulted in dose-dependent and time-dependent growth inhibition in all four gastric cancer cell lines.

Cell viability; 

PubMed: 28139717     


Analysis of tubular cell viability at 24 hours by MTT assay. Mean ± SEM of three independent experiments. *p < 0.001 vs control. 

26965928 28139717
体内研究 在糖尿病ketoacidotic或中性粒细胞减少小鼠中,Deferasirox 显著提高生存率并降低毛霉菌组织的真菌负担,脂质体amphotericin B有类似治疗效果。Deferasirox也增强了宿主对mucormycosis的炎症反应。Deferasirox和脂质体amphotericin B联用时协同提高生存率并降低毛霉菌组织的真菌负担。[1] Deferasirox 口服给药大鼠,至少吸收75%,且生物利用度为26%。Deferasirox(静脉注射和口服)在血液循环主要在不变的形式和其铁络合物存在,Deferasirox有99.2%与血浆蛋白结合。[4] Deferasirox 单药治疗小幅延长小鼠对IPA的生存。[5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 74 mg/mL (198.2 mM)
Water Insoluble
Ethanol ''2 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40% PEG 300+5%Tween 80 +50 % H2O
3.7 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 373.36
化学式

C21H15N3O4

CAS号 201530-41-8
储存条件 粉状
溶于溶剂
别名 CGP-72670

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04423237 Not yet recruiting Drug: Deferasirox Iron Overload University of Pisa|IRCCS Burlo Garofolo|University of Genova June 7 2020 --
NCT03920657 Unknown status Drug: Deferasirox Myelodysplastic Syndromes Fondazione Italiana Sindromi Mielodisplastiche-ETS July 2019 Phase 2
NCT03372083 Completed Drug: Deferasirox Iron Overload Novartis Pharmaceuticals|Novartis January 16 2018 Phase 4
NCT02663752 Terminated Procedure: Bone marrow aspirate|Drug: Deferasirox Myelodysplastic Syndrome Novartis Pharmaceuticals|Novartis May 30 2016 Phase 2
NCT02604433 Active not recruiting Drug: Luspatercept|Other: Placebo Erythrocyte Transfusion|Beta-Thalassemia Celgene|Acceleron Pharma Inc. May 2 2016 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID