Osimertinib (AZD9291; Tagrisso)

Description: Osimertinib (formerly AZD-9291 and mereletinib; trade name Tagrisso) is an oral bioavailable, irreversible/covalent, and mutant-selective EGFR inhibitor with potential antineoplastic activity. It inhibits Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells with IC50s of 12.92, 11.44 and 493.8 nM, respectively. It was approved in 2017 by both FDA and the European Commission for cancer treatment.

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

Related CAS: 1421372-66-8(AZD9291 DA - the des acryl derivative of AZD9291); 1421373-66-1 (mesylate); 1421373-65-0 (free base)

Chemical Name: N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide

InChi Key: DUYJMQONPNNFPI-UHFFFAOYSA-N

InChi Code: InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13, 16-18H, 1, 14-15H2, 2-6H3, (H, 30, 36)(H, 29, 31, 32)

SMILES Code: C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O