EGFR-IN-50 (Compound 9h) 是一种针对 L858R 抗性突变的强效EGFR抑制剂 (TEL-EGFR-L858R-BaF3:GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3:GI50=6.03 μM) 。EGFR-IN-50 表现出对癌细胞的抗增殖活性。

EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI 50 =8 nM, TEL-EGFR-T790M-L858R-BaF3: GI 50 =6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells [1].

EGFR-IN-50 (0-10 μM; 72 h) selectively inhibits NSCLC cell line H3255 (expressing EGFR-L858R) compared to other tumor cells [1]. EGFR-IN-50 (1-10 μM; 72 h) induces cell cycle arrest in G0-G1 phase [1]. EGFR-IN-50 (0.039-10 μM; 4 h) inhibits the phosphorylation of EGFR in H3255 cells [1]. Cell Proliferation Assay [1] Cell Line: A549, H3255, HepG2, MCF-7, HT-29 and A431 cells Concentration: 0-10 μM Incubation Time: 72 hours Result: Showed GI 50 values of >10, and 0.7873 μM for A549 and H3255 cells, respectively. Showed IC 50 values of >10, 7.309, >10 and 6.703 μM for HepG2, MCF-7, HT-29 and A431 cells, respectively. Cell Cycle Analysis [1] Cell Line: H3255 cells Concentration: 1, 5, and 10 μM Incubation Time: 72 hours Result: Increased the percentage of H3255 cells in G0-G1 phase from 60.32% to 88.61%. Western Blot Analysis [1] Cell Line: H3255 cells Concentration: 0.039, 0.15, 0.62, 2.5, and 10 μM Incubation Time: 4 hours Result: Inhibited the phosphorylation of EGFR in H3255 cells in a dose-dependent manner.

2044508-48-5

C24H26BrN3O4S2

564.51

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years