azd9291da

Description: AZD9291-DA (also known as Mutated EGFR-IN-1 or Osimertinib analog) is a des acryl analogue of AZD9291, which is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. AZD9291-DA is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant. AZD9291 is highly active in preclinical models and is well tolerated in animal models. 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.

References: Patent WO 2013014448 A1. 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer; Targeting resistance in lung cancer. Cancer Discov. 2013 Dec; 3(12):OF9. doi: 10.1158/2159-8290.CD-ND2013-025. Epub 2013 Nov 7. PubMed PMID: 24327718.