egfrin9

EGFR-IN-9 is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.

EGFR-IN-91 (compound 9) is an orally active EGFR inhibitor capable of crossing the blood-brain barrier. It effectively inhibits EGFRL858R/C797S and EGFRexon 19del/C797S, leading to tumor regression in patient-derived xenograft (PDX) mouse models. EGFR-IN-91 shows potential for inhibiting locally advanced and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutations.

EGFR-IN-95 is a derivative of 2,4-diaminonicotinamide. It effectively inhibits the activity of EGFRdel19/T790M/C797S and L858R/T790M/C797S.

EGFR-IN-94 (compound 5a) is an EGFR inhibitor with an IC50 of 0.086 μM. It exhibits IC50 values of 0.107 μM for VEGFR-2 and 2.52 μM for Topo II. In HepG-2 cells, EGFR-IN-94 induces apoptosis and causes cell cycle arrest at the S phase.

EGFR-IN-92 (compound 15) is an allosteric inhibitor targeting both T790M and L858R double-mutated EGFR. It exhibits antiproliferative activity against H1975 non-small cell lung cancer (NSCLC) cells expressing these double mutations.

EGFR-IN-93 (compound 18) is an allosteric inhibitor of the T790M/L858R double mutant EGFR. It is applicable for research in non-small cell lung cancer (NSCLC).

EGFR-IN-96 (compound 7a) is a thiophene[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. It causes HepG2 cells to arrest in the S and G2/M phases and inhibits the growth of cancer cells with wild-type EGFR and EGFRT790M.

EGFR-IN-98 (Compound 4c) is an EGFR inhibitor, exhibiting IC50 values of 0.277 μM for L858R/T790M/C797S and 0.089 μM for Del19/T790M/C797S enzymes. It is applicable in tumor research.

EGFR-IN-99 (JBJ-03-142-02) is an EGFR and HER2 Exon 20 insertion mutation inhibitor with antiproliferative activity for the study of non-small cell lung cancer (NSCLC).

EGFR-IN-90 (compound 34), an orally active EGFR inhibitor, demonstrates potent activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and effectively inhibits the proliferation of the H1975-TM cell line carrying EGFRL858R/T790M/C797S mutations with an IC50 of 0.05 μM. Additionally, EGFR-IN-90 suppresses tumor growth in the H1975-TM xenograft tumor model [1].

EGFR-IN-97 (compound 6q), an EGFR inhibitor, demonstrates effectiveness in inhibiting Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, exhibiting IC 50 values of 0.42 μM and 0.41 μM, respectively. Additionally, at a concentration of 0.8 μM, EGFR-IN-97 is capable of inducing apoptosis in NCI-H1975-EGFR L858R/T790M/C797S cells [1].