egfr (l858r/t790m/c797s)

BLU-945 is a reversible, potent, highly selective, and orally available epidermal growth factor receptor tyrosine kinase inhibitor (TKIs). BLU-945 inhibits EGFR phosphorylation in EGFR L858R T790M C797S and EGFR ex19del T790M C797S mutant cell lines. BLU-945 can be used in lung cancer research, including non-small cell lung cancer (NSCLC).

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-120 (Compound 11eg) is an orally effective EGFR inhibitor. It exhibits potency against the EGFR L858R T790M C797S mutant with an IC50 of 0.053 μM, and displays weaker activity against EGFRWT, with an IC50 of 1.05 μM. EGFR-IN-120 inhibits the phosphorylation of EGFR as well as key downstream effectors including STAT3, AKT, and Erk. This compound induces cell cycle arrest and apoptosis in cells harboring the EGFR mutation. Additionally, EGFR-IN-120 inhibits the proliferation of NSCLC cells containing the EGFR L858R T790M C797S mutation, with an IC50 value of 0.052 μM.

EGFR mutant-IN-2 (Compound D51) is an inhibitor of EGFR mutants, specifically targeting EGFR L858R T790M C797S and EGFR del19 T790M C797S mutants with IC50 values of 14 nM and 62 nM, respectively. This compound exhibits favorable pharmacokinetic (PK) parameters, safety properties, in vivo stability, and demonstrates antitumor activity [1].

EGFR-IN-82 (Compound 8a) is a potent, orally active inhibitor of EGFR, exhibiting IC50 values of 0.09 nM for EGFR L858R T790M C797S and 0.06 nM for EGFR Del19 T790M C797S. It lacks significant inhibitory effects on EGFR WT. Demonstrating anti-proliferative properties, EGFR-IN-82 also inhibits tumor growth in nude mice, rendering it applicable in non-small cell lung cancer research [1].

EGFR-IN-22 is a highly effective inhibitor targeting wild type EGFR and its mutant form, EGFR L858R T790M C797S, displaying IC50 values of 4.91 nM and 0.54 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.

EMI1 can be used in the mutant EGFR-associated, drug-resistant non-small-cell lung cancer(NSCLC) research. EMI1 is an inhibitor of EGFR L858R T790M C797S and EGFR ex19del T790M C797S [1].

EGFR-IN-24 is a potent inhibitor of EGFR and inhibits EGFR (del19 T790M C797S) and EGFR (L858R T790M C797S).

EGFR-IN-18 is a potent inhibitor of the enzymatic activity of the L858R T790M C797S mutant EGFR (4.9 nM) and is also able to reduce the enzymatic activity of wild-type EGFR (47 nM).

pan-HER-IN-1 (Compound C5) is an irreversible, orally active Pan-HER inhibitor that exhibits IC50 values of 0.38 nM for EGFR, 1.6 nM for HER4, 2.2 nM for EGFR T790M L858R, and 3.5 nM for HER2, respectively. pan-HER-IN-1 induces apoptosis and demonstrates antitumor activities.

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-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].

EGFR-IN-61 (compound 22a), a potent EGFR kinase inhibitor, exhibits IC50 values of 42 nM for L858R T790M, 137 nM for L858R T790M C797S, and 743 nM for WT. Additionally, it demonstrates antiproliferative activity against the A549 and H1975 cell lines, with IC50 values of 2.14 μM and 1.82 μM, respectively [1].

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-IN-62 is a potent inhibitor of EGFR kinase with IC50 values of 10 nM for L858R T790 M, 29 nM for WT and 2 42 nM for L858R T790 M C797S. EGFR-IN-62 blocks the cell cycle of A549 and or H1975 cells in G1 G0 phase and induces apoptosis and motility inhibition. EGFR-IN-62 effectively inhibited the proliferation of A549 (IC50: 2.53 μM) and H1975 cells (IC50: 1.56 μM).

JBJ-09-063 is a mutant-selective allosteric inhibitor of the epidermal growth factor receptor (EGFR), with potent inhibitory activity demonstrated by half-maximal inhibitory concentrations (IC50s) of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R T790M, 0.083 nM for EGFR L858R T790M C797S, and 0.396 nM for EGFR L747S. This compound effectively decreases phosphorylation of EGFR, Akt, and ERK1 2, showing efficacy in both EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 holds potential for research into EGFR-mutant lung cancer.

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.

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-104 (Compound A23) acts as a potent EGFR inhibitor, demonstrating IC50 values of 0.33 μM for EGFR L858R T790M and 0.133 μM for EGFR Del19 T790M C797S. It exhibits anticancer properties, effective both in vitro and in vivo [1].

LS-106 is an orally active, effective epidermal growth factor receptor (EGFR) inhibitor displaying antitumor activity both in vitro and in vivo. It inhibits the kinase activities of EGFR19del T790M C797S and EGFRL858R T790M C797S, with IC50 values of 2.4 nmol L and 3.1 nmol L, respectively, demonstrating stronger inhibition than Osimertinib. LS-106 induces cell apoptosis (Apoptosis), suppresses the proliferation of tumor cells carrying EGFR19del T790M C797S, and results in significant tumor reduction in a C797S mutant xenograft model.

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-101 (I-10), a 2-phenylamino pyrimidine derivative, is an EGFR inhibitor with IC50 values of 33.26 nM for EGFR L858R T790M C797S and 106.4 nM for Ba F3-EGFR L858R T790M C797S. It is applicable in the study of non-small cell lung cancer (NSCLC) [1].

EGFR-IN-17 is a potent and selective epidermal growth factor receptor (EGFR) inhibitor with an IC50 value of 0.0002 μM, effective in overcoming C797S-mediated drug resistance.