National Yang Ming Chiao Tung University

Jui-I Chao

Kuang-Kai Liu

Jinn-Moon Yang

Ya-Hui Wu

Chin-Piao Chen

Su-Pei Wang

Chinpiao Chen

Ya-Ping Hsu

Kai-Hao Yin

a pharmaceutical composition for preventing, treating, or ameliorating one or more symptoms of a malignant tumor associated with EGFR mutation and/or K-RAS mutation is provided. The pharmaceutical composition includes a 4-anilinoquinazoline derivative having a formula (I) 

4-anilinoquinazoline derivative and albumin conjugates thereof

EGFR mutation (T790M) and cancerous stemness have shown drug resistances in human non-small-cell lung cancer (NSCLC), thus development of novel drugs in overcoming drug resistances in the NSCLC therapy is highly desired. SP101 is a novel gefitinib derivative, which can bind the ATP-binding pocket of EGFR to inhibit its EGFR kinase activity. SP101 can reduce the drug resistances of EGFR mutation (T790M) and cancerous stemness in NSCLC. SP101 induced cancer cell death and apoptosis in the gefitinib-resistant EGFR mutation (T790M) H1975 cells. SP101 inhibited phosphorylated EGFR and its downstream Survivin proteins but conversely induced Caspase 3 activation for apoptosis induction. Moreover, SP101 could decrease Oct4 protein level and reduce Survivin proteins but conversely elicited active Caspase 3 in the xenograft human H1975 lung tumors in nude mice.

Method for overcoming drug resistance of EGFR mutation and cancerous stemness of human non-small cell lung carcinoma

The present invention provides a compound of Formula (I) and a salt thereof, 

Compound for promoting apoptosis of cancer cells and a pharmaceutical composition containing the same and uses thereof

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Zhubei, Taiwan

Jui-I Chao