Lazertinib

Lazertinib is an irreversible inhibitor of mutant EGFRs (IC50s = 1.7, 2, and 3.3 nM for EGFRL858R/T790M, EGFRDel19/T790M, and EGFRDel19, respectively). It is selective for mutant EGFRs over wild-type EGFR, HER2, and HER4 (IC50s = 76, 364, and 1,017 nM, respectively). Lazertinib reduces viability of Ba/F3 cells expressing mutant EGFRs (IC50s = 3.3-5.7 nM). In vivo, lazertinib (1, 3, and 10 mg/kg) reduces tumor volume in an EGFRT790M mutant H1975 non-small cell lung cancer (NSCLC) mouse xenograft model.Formal Name: N-[5-[[4-[4-[(dimethylamino)methyl]-3-phenyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]-4-methoxy-2-(4-morpholinyl)phenyl]-2-propenamide. CAS Number: 1903008-80-9. Synonyms: YH25448. Molecular Formula: C30H34N8O3. Formula Weight: 554.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 3mg/mL, DMF:PBS (pH 7.2) (1:2): 0.3mg/mL, DMSO: 0.2mg/mL. lambdamax: 296 nm. SMILES: COC1=C(NC2=NC=CC(N3N=C(C4=CC=CC=C4)C(CN(C)C)=C3)=N2)C=C(NC(C=C)=O)C(N5CCOCC5)=C1. InChi Code: InChI=1S/C30H34N8O3/c1-5-28(39)32-23-17-24(26(40-4)18-25(23)37-13-15-41-16-14-37)33-30-31-12-11-27(34-30)38-20-22(19-36(2)3)29(35-38)21-9-7-6-8-10-21/h5-12,17-18,20H,1,13-16,19H2,2-4H3,(H,32,39)(H,31,33,34). InChi Key: RRMJMHOQSALEJJ-UHFFFAOYSA-N.