egfr-in-11

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/HER2-IN-11 (compound 20), an orally active dual inhibitor targeting human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), demonstrates IC50 values of 7.7 nM and 22 nM, respectively. This compound shows strong antitumor efficacy, specifically inhibiting the proliferation of BT-474 cancer cells with a GI50 of 601 nM [1].

EGFR-IN-110 (Compound 6) is a covalent inhibitor of EGFR, demonstrating pIC50 values of 9.2 for the EGFR enzyme and 8.7 for EGFR cells. It exhibits strong efficacy in targeting EGFR and maintains good kinase selectivity.

EGFR-IN-116 (compound 14D) is an antineoplastic agent. It exhibits an IC50 value of 0.103 μM for EGFR, 0.069 μM for VEGFR-2, and 19.74 μM for Topo II.

EGFR-IN-115 (H-13) is an EGFR inhibitor with an IC50 value of 395.2 nM and is applicable in cancer research.

EGFR-IN-118 (Compound 4a) is an inhibitor of the tyrosine kinase EGFR. It exhibits anticancer properties, effectively inhibiting the proliferation of MCF-7 and PC3 cells, with IC50 values of 2.53 and 3.25 µg/ml, respectively. Additionally, EGFR-IN-118 demonstrates antioxidant activity by inhibiting DPPH free radicals, with an IC50 of 10.04 µg/ml.

EGFR-IN-112 (SPP10), an EGFR kinase inhibitor, displays IC50 values of 2.31 ± 0.3 μM for MCF-7, 3.16 ± 0.8 μM for H69AR, and 4.2 ± 0.2 μM for PC-3 cancer cells, showcasing selective cytotoxicity towards these cancer cell lines.

EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutations, specifically targeting the tumor environment and inducing apoptosis in cancer cells. This compound effectively inhibits the proliferation of H1975, PC-9, and mutant EGFR cells including BaF3-EGFRL858R/T790M/C797S and BaF3–C797S/Del19/T790M, with IC50 values of 13 nM, 19 nM, 1.2 nM, and 1.3 nM respectively. Additionally, EGFR-IN-117 demonstrates anti-tumor activity in mouse models.

EGFR-IN-119 (Compound 5l) functions as an inhibitor of EGFR with an IC50 of 84.3 nM. It exhibits cytotoxic effects in A549 lung cancer cells with an IC50 of 1.34 μM. Additionally, EGFR-IN-119 downregulates the expression of EGFR, KRAS, and MAP2K genes. It displays antioxidative activity by decreasing reactive oxygen species (ROS) and hyperpolarizing mitochondrial membrane potential.

MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.

EGF Rligand-11, a target protein ligand for EGFR, is utilized in the synthesis of PROTAC MS154.

Tesevatinib tosylate (XL-647 tosylate) is an orally administered epidermal growth factor receptor (EGFR) inhibitor that can cross the blood-brain barrier. It significantly reduces cell viability with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Additionally, Tesevatinib tosylate inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM), demonstrating antitumor activity by inhibiting tumor proliferation.

Afatinib impurity 11 is a byproduct of Afatinib, an irreversible EGFR family inhibitor with IC50 values of 0.5 nM, 0.4 nM, 10 nM, and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M, and HER2, respectively[1].

HSP90-IN-11 is a potent inhibitor of HSP90 and induces significant accumulation of the sub-G1 population. HSP90-IN-11 has a potent HSP90α inhibitory effect comparable to that of AUY-922 (Luminespib). In CRC and NSCLC cells, HSP90-IN-11 exhibited significant anti-proliferative activity in the double-digit nM range.HSP90-IN-11 was able to rapidly degrade client proteins EGFR and Akt in NSCLC cells.