Olafertinib

• CAT Number: I019692
• CAS Number: 1660963-42-7
• Molecular Formula: C₂₉H₂₈F₂N₆O₂
• Molecular Weight: 530.57
• Purity: ≥95%
• Target: Protein Tyrosine Kinase/RTK

Olafertinib (CAT: I019692) is a potent third-generation EGFR TKI (tyrosine kinase inhibitor), demonstrating remarkable inhibitory activity against EGFR mutants L858R/T790M (GI50 = 5 nM) and del19 (GI50 = 10 nM), while also displaying moderate activity against EGFR WT (GI50 = 689 nM). Its mode of action involves targeted inhibition of mutant EGFR variants, suppressing aberrant signaling pathways associated with non-small cell lung cancer (NSCLC). Olafertinib exhibits promising pharmacologic action by selectively impeding oncogenic signaling cascades, making it a potential therapeutic option for NSCLC treatment.

Reference

[1]. Misako Nagasaka, et al. Beyond osimertinib: The development of 3 rd-generation EGFR Tyrosine Kinase Inhibitors. J Thorac Oncol. 2020 Dec 15;S1556-0864(20)31105-9.