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. )

EGFR/C797S-IN-1 is a potent inhibitor targeting the EGFR-C797S mutation, with an IC50 value of 0.128 µM, exhibiting significant anti-proliferative and anti-tumor effects by inhibiting p-EGFR expression in a dose-dependent manner.

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.

PROTACEGFRdegrader 14 is a potent and selective EGFR PROTAC degrader with a DC50 value of approximately 2.9 nM against EGFRL858R/T790M/C797S and a Dmax of 93.1%. It induces the selective degradation of EGFRC797S via a VHL and proteasome-dependent mechanism, downregulating EGFR-related transcriptomes. PROTACEGFRdegrader 14 exhibits high selectivity for EGFRWT, induces cell cycle arrest and apoptosis, and effectively inhibits tumor growth. It is applicable for research on non-small cell lung cancer (NSCLC).

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].