Rogaratinib-BAY1163877-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERogaratinibCat. No.: HY-100019CAS No.: 1443530-05-9Synonyms: BAY1163877分式: CHNOS分量: 466.56作靶點(diǎn): FGFR作通路: Protein Tyrosine Kinase/RTK儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 6 mg/mL (1

2、2.86 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.1433 mL 10.7167 mL 21.4335 mL5 mM 0.4287 mL 2.1433 mL 4.2867 mL10 mM 0.2143 mL 1.0717 mL 2.1433 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Rogaratinib種有效且有選擇性的成纖維細(xì)胞長(zhǎng)因受體 (FGFR) 抑制劑。IC50 & Target FG

3、FR1 FGFR2 FGFR3 FGFR4體外研究Of the 24 cell lines, 2 FGFR1-amplified lung cancer (LC) cell lines, H1581 and DMS114, show extremesensitivity to Rogaratinib (BAY1163877) (GI50 values ranging from 36 to 244nM). Treatment with1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemERogaratinib results in a signific

4、ant decrease in colonies formed by H1581P cells, but not by H1581AR andBR cells. Ectopic expression of Met significantly induces resistance to Rogaratinib in MTT assays. Metoverexpression induces activation of downstream extracellular signal-regulated kinase 1/2 (ERK1/2) andAKT, which cannot be abro

5、gated by Rogaratinib treatment 1.PROTOCOLCell Assay 1 Cells (3000 cells/well) are seeded on 96-well plates at 37C. After overnight incubation, the cells are treatedwith Rogaratinib for 72h. Then, MTT reagent 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide isadded to each well and incubat

6、ed for 4h at 37C. MTT solubilization solution/stop mix is added to each well,mixed, and the plates are incubated overnight at 37C. After measuring the absorbance at 570nm, the dataare graphically displayed 1.MCE has not independently confirmed the accuracy of these methods. They are for reference on

7、ly.戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) IOP Conf Ser Mater Sci Eng. 2019 Aug.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Kim SM, et al. Activation of the Met kinase confers acquired drug resistance in FGFR-targeted lung cancer therapy. Oncogenesis. 2016Jul 18;5(7):e241.McePdfHeightCaution: Product has not been fully validated for medical applications.For research us