Enzyme inhibitor
This orally administered, irreversible pan-Human Epidermal growth factor
Receptor (HER) inhibitor (FWfree-base = 441.28 g/mol), also known by the
code name HM781-36B and systematically as 1-[4-[4- (3,4-dichloro-2-
fluorophenylamino) -7-methoxyquinazolin-6-yloxy]-piperidin-1-yl]prop-2-
en-1-one hydrochloride, is a new anticancer drug intended to treat advanced
solid tumors in clinical trial. HER2-amplified cells were sensitive to
HM781-36B (IC50=1-10 nM), arresting in G1 arrest and undergoing
subsequent apoptosis. HM781-36B shows promise in the treatment for
HER2-amplified breast cancer, especially as a chemosensitizer when used
in combination with other cytotoxic agents (e.g., 5-fluorouracil, cisplatin,
paclitaxel, or gemcitabine).