Mubritinib-TAK-165-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMubritinibCat. No.: HY-13501CAS No.: 366017-09-6Synonyms: TAK-165分式: CHFNO分量: 468.47作靶点: EGFR作通路: JAK/STAT Signaling; Protein Tyrosine Kinase/RTK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 DMS

2、O : 50 mg/mL (106.73 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.34 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.34 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活

3、性 Mubritinib (TAK-165)是有效，选择性的 EGFR2/HER2 抑制剂，IC50 值为6 nM。IC50 & Target HER26 nM (IC50)体外研究 TAK-165 specifically inhibits HER2 tyrosine kinase with an IC50 6 nM and does not inhibit other typestyrosine kinase up to 25 000 nM. TAK-165 inhibits HER2 phosphorylation and its down-stream Akt andMAPK in H

4、ER2 strongly expressing cells (BT474 breast cancer cell line). TAK-165 sensitivity depends onHER2 levels of each cell line. Especially, BT474 cells which over-express HER2 strongly is highly sensitive(IC50=0.005 M) and PC-3 cells which express HER2 very weakly is less sensitive (IC50=4.62 M). But,HT

5、1376 and ACHN cells that over-expressed EGFR showed high IC50 (IC5025 M) 1.体内研究 In the xenograft model, treatment with TAK-165 significantly inhibits growth of UMUC-3, ACHN, and LN-REC4. The antitumor effect after 14 days treatment are 22.9%, 26.0%, and 26.5% in UMUC3, ACHN andLN-REC4, respectively

6、1.PROTOCOLCell Assay 1 Cells are treated with TAK-165 at various concentrations for 72 h. After the incubation period, the cells arecounted. The IC50 value is calculated from a doseresponse curve generated by least-squares linearregression of the response 1.MCE has not independently confirmed the ac

7、curacy of these methods. They are for reference only.Animal Mice: UMUC-3 and LN-REC4 cells are implanted with 50% Matrigel solution. After the tumor volume reachesAdministration 1 200300 mm3 in LN-REC4 and UMUC-3 cells and to 100200 mm3 in ACHN, the mice are treated orallytwice daily for 14 days wit

8、h vehicle (control) or 10 or 20 mg/kg per day of TAK-165. In the Herceptin studyagainst UMUC-3, treatments consist of a twice weekly intraperitoneal injection of 20 mg/kg Herceptin in PBSfor 2 weeks. Tumor growth is assessed by electronic caliper measurement of tumor diameter in twodimensions, and t

9、umor volume is calculated 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.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Nagasawa J, et al. Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEcancer in vitro and in vivo. Int J Urol. 2006 May;13(5):587-92.McePdfHeightCaution: Product has not been fully validated