Bafetinib is a Lyn and Bcr-Abl Tyrosine Kinase Inhibitor
The treatment of Philadelphia chromosome-positive (Ph+) leukemias has improved markedly. There are some inhibitors of Bcr-Abl tyrosine kinase (TK) that are effective for Ph<sup>+</sup> leukemias. However, resistance to imatinib can develop by various molecular mechanisms. They include Bcr-Abl overexpression, mutations within the imatinib-binding site of Bcr-Abl, expression of a...
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...