在外显子19,我们共发现三种框架删除突变,其中最常见的是2235_2249delGGAATTAAGAGAAGC,它直接导致5个氨基酸的缺失(E746_A750del)。外显子18只检测到1例点突变,它导致第719位的甘氨酸为丝氨酸所替代(G719S)(附图)。 突变相关因素 52例腺癌中23例发生突变(44.2%),15例腺鳞癌中3例突变(20%),在所有33例鳞癌...
S1170WZ3146WZ3146是一种突变选择性的,不可逆EGFR(L858R)和EGFR(E746_A750)抑制剂,IC50分别为2 nM和2 nM;对ERBB2磷酸化(T798I)没有抑制作用。 Sci Rep, 2024, 14(1):22895 Aging (Albany NY), 2020, 12(19):19022-19044 S2752HER2-Inhibitor-1HER2-Inhibitor-1是ARRY-380的类似物。ARRY-380是一种...
S1170WZ3146WZ3146 is a mutant-selective irreversible inhibitor ofEGFR(L858R)andEGFR(E746_A750)withIC50of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I). Aging (Albany NY), 2020, 12(19):19022-19044 S2752HER2-Inhibitor-1HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-...
human HCC827 cellsProliferation assay72 hAntiproliferative activity against human HCC827 cells harboring EGFR del E746-A750 mutant after 72 hrs by MTS assay, IC50=0.001 μM22339342 A431 cellsFunction assayInhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immuno...
In the EGFR gene, the most prevalent mutation type was L858R (CTG>CGG) in exon 21, which accounted for 46.5% of all EGFR mutations. Del E746-A750 (K745:AAA), del E746-A750 (K745:AAG), del L747S752 ins S, del L747-E749 ins P and del L747-T751 were the ?ve major in-...