egfrin1

EGFR-IN-1, an orally active and irreversible selective inhibitor targeting L858R/T790M mutant EGFR, exhibits strong antiproliferative and antitumor activity, particularly against H1975 cells and first line mutant HCC827 cells. This compound potently inhibits Gefitinib-resistant EGFR L858R/T790M mutations with a 100-fold selectivity over the wild-type EGFR.

EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR. It exhibits potent antitumor and antiproliferative activity in H1975 cells and mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.

Mutated EGFR-IN-1 (Osimertinib analog) is a valuable intermediate in designing inhibitors for mutated EGFR, including L858R EGFR, Exon19 deletion activating mutant, and T790M resistance mutant.

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-127 is an ATP-competitive inhibitor targeting EGFR, with IC50 values of 136.3 nM for EGFRdel19 and 161.2 nM for EGFRdel19/T790M/C797S. This compound holds potential for the study of non-small cell lung cancer (NSCLC).

EGFR-IN-124 (compound 10A) is an EGFR inhibitor with an IC50 value of 0.54 μM, utilized in cancer research.

EGFR-IN-129 (Compound 10b) is an effective, selective EGFR inhibitor with an IC50 of 51.2 nM and demonstrates broad-spectrum antiproliferative activity against the NCI tumor panel.

EGFR-IN-131 (compound 3a) is an efficacious EGFR inhibitor capable of crossing the blood-brain barrier, with an IC50 value of 272.9 nM. This compound exhibits anti-proliferative activity, induces cellular apoptosis (apoptosis), and causes cell cycle arrest in the G0/G1 phase. Additionally, EGFR-IN-131 reduces the protein expression of p-EGFR.

EGFR-IN-128 (compound 28) is a potent and selective molecule targeting wild-type EGFREx20Ins, demonstrating therapeutic efficacy across various human xenograft models and capable of penetrating the blood-brain barrier in preclinical species.

EGFR-IN-135 (compound 3d) is an EGFR inhibitor with an IC50 value of 0.086 µM. It inhibits cell growth and arrests the cell cycle in the S phase in breast cancer cell lines.

EGFR-IN-134 (compound 3f) is a triazolo[3,4-a]quinoline derivative and functions as a potent EGFR inhibitor with an IC50 of 0.023 µM. It induces apoptosis and necrosis in cells, and causes cell cycle arrest in the G2/M and pre-G1 phases. EGFR-IN-134 modulates the expression of apoptosis-regulating proteins by downregulating anti-apoptotic protein Bcl2 and upregulating pro-apoptotic proteins p53, Bax, and caspases 3, 8, and 9, demonstrating significant antiproliferative and anticancer activities.

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-130 (compound 14b) is an EGFR inhibitor and an inducer of apoptosis (apoptoosis). It effectively kills HeLa cancer cells by inducing apoptosis.

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-137 (Compound 4c) acts as an inhibitor of aromatase and EGFR, with IC50 values of 1.67 μg/mL and 0.08 μg/mL, respectively. It hinders the proliferation of cancer cells MCF-7 and MDA-MB-231, with IC50 values of 1.62 µM and 4.14 µM. Additionally, EGFR-IN-137 induces cell cycle arrest at the G0/G1 phase in MDA-MB-231 cells and triggers apoptosis through a caspase-dependent pathway.

EGFR-IN-138 (compound 19) is a potent inhibitor of EGFR, with IC50 values of 37, 2.6, and 1.9 nM for the wild-type, L858R, and T790M EGFR, respectively.

EGFR-IN-142 (compound 9a) is an EGFR inhibitor with an IC50 value of 0.08 μM. It exhibits antiproliferative activity against MCF-7 cells (IC50 = 3.31 μM) and WI-38 cells (IC50 = 43.99 μM).

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-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, it inhibits wild-type EGFR kinase by 52.7%.

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-144 (Compound 4B) inhibits EGFR (IC50=0.639 µg/mL) and tubulin polymerization (IC50=7.339 µg/mL). It exhibits cytotoxicity in various cancer cells with a GI50 at the nanomolar level. EGFR-IN-144 reduces the expression of mTOR, TNF-α, and IL-6, causes G1/S phase cell cycle arrest, and induces apoptosis.

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).