osimertinib-dimesylate

Description: Osimertinib dimesylate (formerly known as AZD-9291 dimesylate and mereletinib dimesylate) is a novel, potent, oral bioavailable, irreversible, and mutant-selective, 3rd generation EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. It inhibits both activating and resistant EGFR mutations while sparing the normal form of EGFR that is present in normal skin and gut cells, thereby reducing the side effects encountered with currently available medicines. It was approved as a cancer treatment in 2017 by both the Food and Drug Administration and the European Commission.

References: Transl Lung Cancer Res. 2014 Dec; 3(6):370-2; J Med Chem. 2014 Oct 23; 57(20):8249-67.

Related CAS: 1421373-66-1 (mesylate); 1421372-66-8 (AZD9291 DA - the des acryl derivative of AZD9291); 1421373-66-1 (mesylate)