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.

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).

HG-14-10-04 is a potent and specific ALK (anaplastic lymphoma kinase) inhibitor.

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].

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-47 is a potent, orally active inhibitor of EGFRL858R T790M C797S (IC50: 0.01 μM). EGFR-IN-47 is capable of blocking the cell cycle and inducing apoptosis. EGFR-IN-47 has potential for NSCLC studies.

EGFR kinase inhibitor 1 is a potent inhibitor of EGFR that acts on WT (IC50: 37 nM), l885R T790M (IC50: 1.7 nM), and L858R T790M C797S (IC50>300 nM). It is capable of blocking the cell cycle in G0 G1 phase, inducing apoptosis, and has an inhibitory effect on cell metastasis. Additionally, EGFR kinase inhibitor 1 exhibits anti-proliferative and anti-tumor effects.

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

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-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.

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).

EGFR-IN-48 is a potent, orally active EGFR inhibitor that acts on EGFRd19 TM CS (IC50: 0.193 nM), EGFRLR TM CS (IC50: 0.251 nM), EGFRWT (IC50: 10.4 nM). EGFR-IN-48 is also able to inhibit EGFR-IN-48 also inhibits the proliferation of BaF3EGFR del19 T790M C797S cells (IC50: 1.526 nM) and PC-9EGFR del19 T790M C797S cells (IC50: 66.7 nM).

JBJ-09-063 hydrochloride is an EGFR inhibitor selective for mutants, demonstrating IC50 values of 0.147 nM, 0.063 nM, 0.083 nM, and 0.396 nM against EGFR L858R, EGFR L858R T790M, EGFR L858R T790M C797S, and EGFR L747S, respectively. It effectively inhibits EGFR, Akt, and ERK1 2 phosphorylation, showing efficacy in both EGFR tyrosine kinase inhibitor (TKI)-sensitive and -resistant models. This compound holds potential for research on EGFR-mutant lung cancer.