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Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M).

Osimertinib dimesylate is a novel oral, selective inhibitor of MET protein tyrosine kinase. It has been shown to be selectively toxic to tumor cells that express the MET protein tyrosine kinase and is an effective agent for the treatment of metastatic and/or locally advanced solid tumors. Osimertinib dimesylate has been shown to inhibit tumor growth in vivo in xenograft models, including those with acquired resistance to other agents. MET inhibition has been shown to cause tumor regression in some cases. The molecular target of osimertinib dimesylate is the MET receptor tyrosine kinase, which is overexpressed in many cancers. MET inhibition leads to downstream signaling events leading to cell cycle arrest and apoptosis induction. The drug also inhibits RNA synthesis by binding directly to ribosomes as well as DNA synthesis by binding directly to DNA polymerases, resulting in a potent antitumor activity against various cancer types