Olafertinib 是新型突变选择性、不可逆、可口服的EGFR酪氨酸酶抑制剂，可克服 NSCLC 中 T790M 介导的耐药性。

CK-101 (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.

CK-101 specifically targets the mutant forms of EGFR, including T790M, while exhibiting minimal activity toward WT EGFR. It selectively inhibits cell proliferation of cell lines expressing both the activating (HCC827, IC50<15 nM) and resistance mutations (NCI-H1975, IC50<5 nM).

CK-101 significantly inhibits tumor growth in EGFR-mutated NSCLC tumor xenograft models, with no activity in the WT EGFR tumor xenograft model.

1660963-42-7

C29H28F2N6O2

530.57

CK-101;RX-518;EGFR-IN-3

H2O:Insoluble
DMSO:120 mg/mL (226.18 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years