egfr (l858r/t790m/c797s)

EGFR-IN-11 is a selective inhibitor of EGFR-tyrosine kinase and induces cell apoptosis. EGFR-IN-11 inhibits triple mutant EGFRL858R/T790M/C797S with an IC50 of 18 nM and arrests cell cycle at G0/G1.

EGFR-IN-5 is a selective inhibitor of EGFR. The IC50s for EGFR, EGFR(L858R), EGFR(L858R/T790M), and EGFR(L858R/T790M/C797S) are 10.4, 1.1, 34, 7.2 nM, respectively.

EGFR mutant- in-1, A 5-methylpyrimidopyridone derivative are effective selective EGFRL858R/T790M/C797S mutant inhibitors with IC50 of 27.5 nM, which significantly weakened EGFRWT effect.

EGFR-IN-7 (TQB3804) is a selective and potent EGFR kinase inhibitor.

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-IN-126 (compound 9d) is an effective inhibitor of EGFR L858R/T790M/C797S, displaying an IC50 value of 0.005 μM. It exhibits antitumor activity both in vivo and in vitro.

EGFR-IN-132 (Compound 23) is an EGFR inhibitor effective against various EGFR mutations including the wild-type, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S with IC50 values of 1.6, 0.025, 0.019, 0.022, and 0.029 nM, respectively. This compound demonstrates favorable pharmacokinetics with high oral bioavailability.

EGFR-IN-133 (Compound 24) serves as an inhibitor targeting various mutations of the EGFR, including the wild type, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S with respective IC50 values of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. The compound exhibits favorable pharmacokinetic properties and high oral bioavailability.

EGFR-IN-140 (Compound 31) is an inhibitor of EGFR, effectively targeting both wild-type EGFR and the EGFRL858R/T790M/C797S mutant, with Ki values of 0.95 nM and 2.1 nM, respectively. Additionally, it inhibits EGFRdel19/T790M/C797S in Ba/F3 cells with an IC50 of 56.9 nM and demonstrates antitumor activity in mouse models.

EGFR-IN-125 (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM for EGFR(d746-750/T790M/C797S), 0.52 nM for EGFR(L858R/T790M/C797S), 0.5 nM for EGFR(d746-750/C797S), 0.69 nM for EGFR(L858R/C797S), and 0.92 nM for EGFR (wild type).

LSD1/EGFR-IN-1 (compound L-1) is an effective inhibitor of LSD1, EGFRT790M/L858R, and EGFRL858R/T790M/C797S, with IC50 values of 6.24, 2.06, and 5.01 μM, respectively. This compound plays a significant role in cancer research.

EGFR-IN-136 (compound 21v) is a potent inhibitor of EGFR, demonstrating IC50 values of 20.2 nM, 1.2 nM, 2.3 nM, and 12.5 nM for EGFRWT, EGFRLR/TM, EGFR19D/TM/CS, and EGFRLR/TM/CS, respectively. It exhibits antiproliferative and antitumor activities and holds potential for research in non-small cell lung cancer (NSCLC).

EGFR-IN-139 (compound PD 18) is an EGFR inhibitor with IC50 values of 12.88 nM (wild type), 10.84 nM (L858R/T790M), and 42.68 nM (L858R/T790M/C797S). It demonstrates significant anticancer activity against the A549 and H1975 cancer cell lines, which express high levels of EGFR. EGFR-IN-139 exhibits strong selectivity for cancer cells and can be utilized in research on non-small cell lung cancer (NSCLC).

EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of the L858R/T790M/C797S mutant EGFR kinase, with an IC50 value of 0.87 nM. EGFR-IN-161 effectively inhibits tumor cell apoptosis, G1 phase arrest, and migration.

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-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.

ZSH-2117 is a covalent and selective EGFR PROTAC degrader, with a DC50 of 45 nM in Ba/F3-EGFR[L858R/T790M/C797S] cells. It significantly inhibits cell proliferation and reduces AKT and ERK protein levels in downstream EGFR signaling pathways. ZSH-2117 effectively suppresses tumor growth in Ba/F3-EGFR[L858R/T790M/C797S] xenograft mouse models.

EGFR-IN-164 (Compound 4) is a selective covalent allosteric inhibitor of EGFR. It effectively inhibits the activity of EGFR^L858R/T790M/C797S kinase with an IC50 of 48.1 nM and suppresses the proliferation of EGFR-mutant cells. EGFR-IN-164 is applicable in research focused on cancer resistance.

PROTACEGFRdegrader 13 (compound 106) is an EGFR PROTAC degrader with a DC50 of less than 0.1 μM. It demonstrates antiproliferative activity against Ba/F3-TEL-EGFR-T790M-L858R-C797S cells, with an IC50 of 15.6 nM. PROTACEGFRdegrader 13 is applicable in the research of EGFR-related diseases, such as cancer.

EGFR-IN-172 is an EGFR inhibitor that effectively suppresses the proliferation of non-small cell lung cancer (NSCLC) cells with L858R, T790M, and C797S drug-resistant mutations. It inhibits the phosphorylation of EGFR, leading to cell cycle arrest and apoptosis. EGFR-IN-172 is suitable for NSCLC research.

EGFR-IN-173 is an orally active, broad-spectrum mutant EGFR tyrosine kinase inhibitor that targets EGFR19del, L858R/T790M, and the triple mutation C797S, with an IC50 of 1.19 nM, effectively inhibiting the EGFR19del/T790M/C797S mutant. It demonstrates over 100-fold selectivity for mutated EGFR compared to the wild type [wild type IC50= 19.362 μM]. EGFR-IN-173 significantly suppresses cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells, inhibits EGFR phosphorylation, and blocks downstream pathways (MAPK/ERK, AKT, STAT3). It shows antitumor activity in NSCLC and Ba/F3 xenograft models and is applicable in NSCLC research.

EGFR-IN-179 (Compound 8d) is an EGFR inhibitor with an IC50 of 0.068 μM for EGFRL858R/T790M/C797S and 2.56 μM for EGFR-WT-TK. It exhibits anticancer activity against non-small cell lung cancer.

EGFR-IN-152 (compound D4) is a potent inhibitor of the EGFR tyrosine kinase and exhibits significant inhibitory activity against the EGFRL858R/T790M/C797S mutations (IC50= 40 nM). It induces cell cycle arrest at the G0/G1 phase and apoptosis, thereby hindering the clonogenic growth and proliferation of non-small cell lung cancer (NSCLC) cells. EGFR-IN-152 is applicable for NSCLC research.

BI-8128 is a potent EGFR inhibitor with IC50 values of 12, 6.7, 22, 10, and 3 nM for wild-type EGFR and the T790M, C797S, T790M/C797S, and L858R/T790M/C797S mutant forms, respectively. It significantly inhibits the proliferation of Ba/F3 and PC-9 cells with resistant mutations. BI-8128 is applicable for research in non-small cell lung cancer.