Osimertinib (AZD9291) is an oral, irreversible, and mutant-selectiveEGFRinhibitor withIC50of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3. In vitro
AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro.
In vivo
AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo. Cell Data
1.Xin Zhang, Yuhan Jiang, Na Guo, Yifan Ding, Jingting Feng, Chenyang Miao, Yanni Lv. (2023) Application of SNAP-tag-EGFR cell membrane chromatography model in screening antitumor active components of Silybum marianum (L.) Gaertn. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, (115816). [PMID:37976988]
References
1.Xin Zhang, Yuhan Jiang, Na Guo, Yifan Ding, Jingting Feng, Chenyang Miao, Yanni Lv. (2023) Application of SNAP-tag-EGFR cell membrane chromatography model in screening antitumor active components of Silybum marianum (L.) Gaertn. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, (115816). [PMID:37976988]
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