Olafertinib

Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies^[1][2]. IC50 & Target:GI50: 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19), 689 nM (EGFR WT)^[1]. In Vitro:Olafertinib (Compound CK-101) (72 h) selectively inhibits cell proliferation of cell lines expressing both the activating (e.g. HCC827, IC₅₀ < 0.015 μM) and resistance mutations (NCI-H1975, IC₅₀ < 0.005 μM)^[2].
In Vivo:Olafertinib (Compound CK-101) (p.o., daily for 14 or 21 days) significantly inhibits tumor growth in EGFR-mutated NSCLC tumor xenograft mice models^[2].
Olafertinib inhibits tumor growth by up to 90% in a xenograft study of PC-9 cells in SCID/Beige mice^[2].
Olafertinib inhibits tumor growth by up to 95% in a xenograft study of NCI-H1975 cells in BALB/c nude mice^[2].