egfrc797s

Mutated EGFR-IN-3 is a ATP-competitive and highly selective allosteric dibenzodiazepinone EGFR(L858R T790M) and EGFR(L858R T790M C797S) inhibitor(IC50 of 12 nM and 13 nM, respectively. )

JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R T790M C797S, EGFRWT and EGFRL858R 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.

EGFR-IN-78 (compound A5), a 2-aminopyrimidine derivative, serves as a reversible EGFR C797S-TK inhibitor and an apoptosis inducer. It exhibits anti-proliferative properties, impedes EGFR phosphorylation, and induces G2 M phase cell cycle arrest [1].

Os30 is a potent fourth-generation EGFR inhibitor, specifically targeting the EGFRC797S-TK mutation with IC50 values of 18 nM for EGFRDel19 T790M C797S TK and 113 nM for EGFRL858R T790M C797S TK. It effectively suppresses EGFR phosphorylation, induces G1 phase arrest, and triggers apoptosis in KC-0116 (BaF3-EGFRDel19 T790M C797S) cells. Moreover, Os30 demonstrates strong antitumor activity in non-small cell lung cancer (NSCLC) harboring the EGFmRC797S mutation [1].