EGFR-IN-204 (Example 1) is a HER2 exon 20 mutation inhibitor with selectivity for wild-type EGFR. EGFR-IN-204 exerts antiproliferative effects on cells dependent on HER2 exon 20 YVMA insertion mutation and wild-type HER2, and shows strong selectivity over cells dependent on wild-type EGFR. EGFR-IN-204 is applicable to non-small cell lung cancer research [1].
In Vitro, EGFR-IN-204 (72 h) exerts antiproliferative effects on HER2 wild-type-dependent Ba/F3 cells, with a GI50 of 9.3 nM[1]. EGFR-IN-204 (72 h) exerts antiproliferative effects on Ba/F3 cells dependent on the HER2 exon 20 YVMA insertion mutation, with a GI50 of 10.3 nM[1].
References:
[1]. Yang, et al. Crystalline form of quinazoline derivative and preparation method therefor. WO2025067398A1. WIPO (PCT). 2024-09-27.
In Vitro, EGFR-IN-204 (72 h) exerts antiproliferative effects on HER2 wild-type-dependent Ba/F3 cells, with a GI50 of 9.3 nM[1]. EGFR-IN-204 (72 h) exerts antiproliferative effects on Ba/F3 cells dependent on the HER2 exon 20 YVMA insertion mutation, with a GI50 of 10.3 nM[1].
References:
[1]. Yang, et al. Crystalline form of quinazoline derivative and preparation method therefor. WO2025067398A1. WIPO (PCT). 2024-09-27.