JND3229

JND3229 is a reversible EGFR^C797S inhibitor with IC₅₀ values of 5.8, 6.8 and 30.5 nM for EGFR^{L858R/T790M/C797S}, EGFR^WT and EGFR^L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma^[1]. IC50 & Target:IC50: 5.8 nM (EGFR^{L858R/T790M/C797S}), 6.8 nM (EGFR^WT), 30.5 nM (EGFR^L858R/T790M)^[1]. In Vitro:JND3229 potently inhibits the proliferation of BaF3 cells (harboring the EGFR^{L858R/T790M/C797S} and EGFR^{19D/T790M/C797S}mutations), NCI-H1975 NSCLC cells (with EGFR^T790M mutation) and A431 cancer cells (overexpressing EGFR^WT) with IC₅₀ values of 0.51, 0.32, 0.31 and 0.27 µM, respectively^[1].
JND3229 (0.1, 0.3, 1, 3, 10 µM; 2 h) potently inhibits the phosphorylation of EGFR^{L858R/T790M/C797S} and EGFR^{19D/T790M/C797S} in engineering BaF3 cells^[1]. In Vivo:JND3229 (10 mg/kg; i.p.; twice daily for 10 days) exhibits an obvious suppression of tumor growth, and shows target inhibition in vivo^[1].