下载本文档
版权说明:本文档由用户提供并上传,收益归属内容提供方,若内容存在侵权,请进行举报或认领
文档简介
1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE3-AminocholestaneCat. No.: HY-19776CAS No.: 2206-20-4分式: CHN分量: 387.68作靶点: Phosphatase作通路: Metabolic Enzyme/Protease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 Ethanol : 50 mg/mL (128.97 mM; N
2、eed ultrasonic)DMSO : 1 mg/mL (insoluble or slightly soluble)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5794 mL 12.8972 mL 25.7945 mL5 mM 0.5159 mL 2.5794 mL 5.1589 mL10 mM 0.2579 mL 1.2897 mL 2.5794 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。BIOLOGICAL ACTIVITY物活性 3-Aminocholestane是含有选
3、择性 SH2 结构域的肌醇-5-磷酸酶 1 (SHIP1) 的抑制剂,其 IC50 值约为 2.5 M。IC50 & Target IC50: 2.5 M (SHIP1) 1体外研究OPM2 cell viability is effectively reduced by 3-Aminocholestane (3AC) treatment. RPMI8226 and U266 cells1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEshow significantly less sensitivity to 3-Aminocholestane
4、 treatment when compare with OPM2 cells, althoughviability is decreased significantly at concentrations of 12.5 M. Treatment with 3-Aminocholestane for 36h severely reduces the percentage of cells in the S phase, which is accompanied by an increase of cells inthe G2/M phase. In contrast, in the less
5、 proliferative RPMI8226 and U266 cells, cell cycle progression isblocked in the G0/G1 phase upon 3-Aminocholestane treatment, in conjunction with a reduced percentageof cells undergoing the S phase 2.体内研究 It is found that 3-Aminocholestane (3AC) results in reduced multiple myeloma (MM) growth in viv
6、o, asdetermined by quantitation of free human Ig light chain in the plasma after OPM2 challenge. In addition,reduced numbers of circulating OPM2 cells, as determined by human HLA-ABC staining, is observed inperipheral blood from 3-Aminocholestane-treated mice compare with vehicle controls. Most impo
7、rtantly, 3-Aminocholestane treatment results in significantly enhanced survival of mice after tumor challenge. In 3-Aminocholestane-treated mice that resist treatment, it is found that MM tumors exhibit an upregulation ofSHIP2, reminiscent of in vitro treatment of OPM2 cells and suggesting that SHIP
8、1 inhibition may select fortumor cells with increased SHIP2 expression 2.PROTOCOLCell Assay 2 Cells are treated in triplicate or more with increasing concentrations of compounds (including 3-Aminocholestane). Cell viability is determined with a Cell Counting Kit according to the manufacturersinstruc
9、tions. The odds density (OD) of compound (including 3-Aminocholestane )-treated cells is divided bythe OD of their vehicle control, and the viability is expressed as a percentage of untreated cells. Results areexpressed as meanstandard error of the mean (SEM) of three individual experiments. For pho
10、sphatidylinositol phosphates (PIP) add-back experiments, MCF-7 cells are treated for 2 h with 10 M SHIP inhibitors(including 3-Aminocholestane ), after which cells are washed and fresh medium is added. Cells aresubsequently cultured in the absence (0 M) or presence (10 or 20 M) of either PtdIns(3,4)
11、P2-diC16 (P-3416) or PtdIns(3,5)P2-diC16 (P-3516) for 36 h, after which cell viability is determined by the Cell CountingKit 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal NOD/SCID/cIL2R (NSG) mice are injected intraperitoneally with 1107 OPM2
12、 cells and 6 h later receive anAdministration 2 initial injection of 3-Aminocholestane (3AC) or vehicle. 3-Aminocholestane is suspended in a 0.3%Klucel/H2O solution at 11.46 mM and administered by intraperitoneal injection of 100 L solution. Vehicle-treated mice receive 100 L injection of 0.3% Kluce
13、l/H2O solution. The mice are then treated with 3-Aminocholestane or vehicle daily for the next 6 d and then twice per week in the remaining 15 wks of thesurvival study 2.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 Oxid Med Cell Longev. 2
14、019 Apr.See more customer validations on HYPERLINK / www.MedChemE2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEREFERENCES1. Chen Z, et al. Signalling thresholds and negative B-cell selection in acute lymphoblastic leukaemia. Nature. 2015 May21;521(7552):357-61.2. Gwenny M Fuhler, et al. Therapeutic Potential of SH2 Domain-Containing Inositol-5-Phosphatase 1 (SHIP1) and SHIP2 Inhibition inCancer. Mol Med. 2012 F
温馨提示
- 1. 本站所有资源如无特殊说明,都需要本地电脑安装OFFICE2007和PDF阅读器。图纸软件为CAD,CAXA,PROE,UG,SolidWorks等.压缩文件请下载最新的WinRAR软件解压。
- 2. 本站的文档不包含任何第三方提供的附件图纸等,如果需要附件,请联系上传者。文件的所有权益归上传用户所有。
- 3. 本站RAR压缩包中若带图纸,网页内容里面会有图纸预览,若没有图纸预览就没有图纸。
- 4. 未经权益所有人同意不得将文件中的内容挪作商业或盈利用途。
- 5. 人人文库网仅提供信息存储空间,仅对用户上传内容的表现方式做保护处理,对用户上传分享的文档内容本身不做任何修改或编辑,并不能对任何下载内容负责。
- 6. 下载文件中如有侵权或不适当内容,请与我们联系,我们立即纠正。
- 7. 本站不保证下载资源的准确性、安全性和完整性, 同时也不承担用户因使用这些下载资源对自己和他人造成任何形式的伤害或损失。
最新文档
- 2024至2030年中国商业地产市场发展预测及投资策略分析报告
- 2024至2030年全国各地区污水处理能力分析报告
- 2024至2030年中国玻璃市场前景及投资机会研究报告
- 2024至2030年中国多功能嵌入式烤箱市场现状研究分析与发展前景预测报告
- 煤炭制品质量保障体系与质量控制考核试卷
- 乐器零售业的人力资源培训与发展体系建设考核试卷
- 家庭寄养与收养儿童的心理适应考核试卷
- 物流学生实习报告范文汇编6篇
- 2024年妊娠诊断制剂项目发展计划
- 2024年工商用制冷、空调设备合作协议书
- 高新技术企业认定中的财务风险及策略
- 《地理信息系统概论》教案
- 15D500-15D505 防雷与接地图集(合订本)
- 招聘app开发方案
- 结膜肿物的治疗及护理
- 综掘机、综掘工艺专项安全风险辨识评估报告
- 《五官科健康教育》课件
- 基层工会内部控制制度范文五篇
- 各国见面礼仪英文版
- 施耐德atsD型控制器用户手册
- 小学班会 九一八事变主题班会 课件 (38张PPT)
评论
0/150
提交评论