| 产品描述： | EGFR/ErbB1 选择性抑制剂 | 活化剂;EGFR/ErbB1 Selective Inhibitors | Activators;;InformationAZD3759 is a potent, oral active, CNS-penetrantEGFRinhibitor withIC50of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. Phase 1.TargetsEGFR (L858R) (Cell-free assay); EGFR (exon 19Del) (Cell-free assay); EGFR (WT) (Cell-free assay) 0.2 nM; 0.2 nM; 0.3 nMIn vitroIn H3255 (L858R) cells, AZD3759 inhibits EGFR phosphorylation with IC50 of 7.2 nM. AZD3759 demonstrates inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255 with IC50 of 7.7 nM and 7 nM, respectively, showing mo activity on cell proliferation of H838 cells.In vivoAZD3759 shows good oral bioavailability in dogs, and penetrates extensively into monkey brain. In a brain metastasis PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) causes significant dose-dependent antitumor efficacy.Cell Research(from reference)Cell lines：PC-9 (exon 19Del), H3255 (L858R) and H838 (wt) cells Concentrations：~30 mM Incubation Time：72 h |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京