| 产品描述： | EGFR/ErbB1 选择性抑制剂 | 活化剂;EGFR/ErbB1 Selective Inhibitors | Activators;;InformationAZ5104, the demethylated metabolite of AZD-9291, is a potentEGFRinhibitor withIC50of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.TargetsEGFR (L858R/T790M) ; EGFR (L861Q) ; EGFR (L858R) ; ErbB4 ; EGFR (wildtype) 15117,<1 nM; 1 nM; 6 nM; 7 nM; 25 nMIn vitroAZ5104 shows great potency against ex19del (2 nM in PC-9), T790M (2 nM in H1975), and wild-type EGFR (33 nM in LOVO) cell lines. AZ5104 causes inhibition of cell viability with IC50 of 3.3 nM, 2.6 nM, 80 nM, and 53 nM for H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT), respectively.In vivoIn both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression.Cell Research(from reference)Cell lines：H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT) cells Incubation Time：96 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