Tag: Autophosphorylation

AG-494 is a Potent and Selective EGFR Inhibitor

Epidermal growth factor (EGF) receptor (EGFR), is the prototype of the EGFR family that also includes ErbB2/HER2/Neu, ErbB3/HER3, and ErbB4/HER4. EGFR is commonly upregulated in cancers such as in non-small-cell lung cancer, metastatic colorectal cancer, glioblastoma, head and neck cancer, pancreatic cancer, and breast cancer. Various mechanisms mediate the upregulation...

PKI-166 is a Selective and Orally Bioavailable EGFR Autophosphorylation Inhibitor

Human pancreatic cancer cells can secrete the proangiogenic molecules, such as VEGF, IL-8, and basic fibroblast growth factor. VEGF is the major proangiogenic factor in most types of human cancer. Therefore, in this article, we will introduce a potent, selective and orally active EGFR tyrosine kinase inhibitor, PKI-166. Firstly,...

CH6953755 is an Orally Active and Selective YES1 Kinase Inhibitor

There are reports of YES1 participating in numerous signaling pathways. SRC is a nonreceptor protein tyrosine kinase and is encoded by a proto-oncogene. Besides, the nine members of the SRC family include YES1, SRC, FYN, LYN, and LCK, have various important cellular functions. Moreover, down-regulating YES1 by short hairpin...