TAK-901 _Aurora Kinase 抑制剂 - MedChemExpress_第1页
TAK-901 _Aurora Kinase 抑制剂 - MedChemExpress_第2页
TAK-901 _Aurora Kinase 抑制剂 - MedChemExpress_第3页
TAK-901 _Aurora Kinase 抑制剂 - MedChemExpress_第4页
全文预览已结束

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.MedChemETAK-901Cat. No.: HY-12201CAS No.: 934541-31-8分式: CHNOS分量: 504.64作靶点: Aurora Kinase作通路: Cell Cycle/DNA Damage; Epigenetics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 : 2 mg/mL (3.96 mM; Ne

2、ed ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9816 mL 9.9081 mL 19.8161 mL5 mM - - -10 mM - - -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 TAK-901是多靶点的的极光激酶 (aurora)抑制剂,对极光激酶A和B的IC50 值分别为21 和15 nM。IC50 & Target Aurora A Aurora B21 nM (IC50) 15

3、nM (IC50)体外研究TAK-901 exhibits time-dependent, tight-binding inhibition of Aurora B, but not Aurora A. Consistent withAurora B inhibition, TAK-901 suppresses cellular histone H3 phosphorylation and induces polyploidy. In1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEvarious human cancer cell lines,

4、 TAK-901inhibits cell proliferation with effective concentration values from 40to 500 nM. Examination of a broad panel of kinases in biochemical assays reveals inhibition of multiplekinases. However, TAK-901 potently inhibits only a few kinases other than Aurora B in intact cells, includingFLT3 and

5、FGFR2 1.体内研究 In rodent xenografts, TAK-901 exhibits potent activity against multiple human solid tumor types, andcomplete regression is observed in the ovarian cancer A2780 model. TAK-901 also displayed potent activityagainst several leukemia models. TAK-901 induces pharmacodynamic responses consist

6、ent with Aurora Binhibition and correlating with retention of TAK-901 in tumor tissue 1.PROTOCOLKinase Assay 1 Enzyme activities of Aurora A/TPX2 and Aurora B/INCENP complexes are assayed at room temperature inbuffer containing serially diluted TAK-901, and the product is quantified using IMAP detec

7、tion reagents.Aurora A/TPX2 (2 nM) is assayed with 100 nM FL-Kemptide and 1 mM ATP. Aurora B/INCENP (0.8 nM) isassayed with 100 nM 5-carboxy-fluorescein-GRTGRRNSI-NH2 (FL-PKAtide) and 10 mM ATP. For time-dependent inhibition, Aurora B/INCENP is incubated with TAK-901 for 1 hour at room temperature f

8、ollowedby addition of 150 mM ATP to initiate the reaction 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 Cells are plated in 96-well microtiter plates and incubated with serial dilutions of TAK-901 for 72 hours. Cellproliferation is dete

9、rmined by ELISA analysis of bromodeoxyuridine (BrdUrd) incorporation into DNA. IMR-90immortalized lung fibroblasts are seeded in 96-well microtiter plates and cultured for 3 to 4 days untilconfluent. Cells are then incubated with serial dilutions of TAK-901 for 72 hours. The MTS assay isconducted 1.

10、MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Tumor-bearing mice or rats are treated intravenously twice daily (b.i.d.) with either vehicle or TAK-901Administration 1 on 2 consecutive days per week or every other day for 2 or 3 cycles. Th

11、e antitumor activity of TAK-901 inhuman tumor and leukemia xenograft models are monitored 1.Nude rats bearing A2780 tumors averaging 250 to 500 mg receive an intravenous dose of TAK-901. Plasmasamples are collected by terminal cardiac puncture under CO2 anesthesia. Tumors are dissected and snap-froz

12、en at -80C 1.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 Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Technical University of Munich. 24.01.2018.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Farrell P, et al. Biological characterization of TAK-901, an investigational, novel, multitargeted Aurora B kinase inhibitor. Mol CancerTher. 2013 Apr;12(4):460-70.McePdfHeight

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。

评论

0/150

提交评论