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

EGFR/ErbB-2 inhibitor-1 is a selective ErbB2/HER2 inhibitor that effectively blocks ErbB2 and HER2 signaling.

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-3 is an EGFR inhibitor with potential antitumour activity.EGFR-IN-3 inhibits EGFRwt-TK and induces apoptosis (cell death), which can cause cells to block in the G2/M phase.

EGFR-IN-99 (JBJ-03-142-02) is an EGFR and HER2 Exon 20 insertion mutation inhibitor with antiproliferative activity for the study of non-small cell lung cancer (NSCLC).

EGFR-IN-9 is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.

CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase (IC50s: 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases).

Cetuximab (C225) is a monoclonal antibody that is an inhibitor of human epidermal growth factor receptor (EGFR) (Kd=0.201 nM). Cetuximab has antitumor activity, inhibiting tumor cell proliferation and inducing apoptosis.

EGFR-IN-90 (compound 34), an orally active EGFR inhibitor, demonstrates potent activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and effectively inhibits the proliferation of the H1975-TM cell line carrying EGFRL858R/T790M/C797S mutations with an IC50 of 0.05 μM. Additionally, EGFR-IN-90 suppresses tumor growth in the H1975-TM xenograft tumor model [1].

PROTAC EGFR degrader 8 (T-184) is a PROTAC that selectively degrades the epidermal growth factor receptor (EGFR) with a DC50 of 15.56 nM in HCC827 cells. It effectively inhibits the growth of various cell lines, including H1975, PC-9, and HCC827, with IC50 values of 7.72 nM, 121.9 nM, and 14.21 nM, respectively. This compound is primarily used for cancer research, particularly in the context of non-small cell lung cancer (NSCLC) [1].

PROTAC EGFR degrader 4 is a potent molecule designed to target and degrade mutant EGFR, showcasing its effectiveness by inducing degradation of EGFR del19 and EGFR L858R/T790M with DC50 values of 0.51 nM and 126 nM, respectively. Furthermore, it significantly inhibits the growth of HCC827 and H1975 cell lines, demonstrating IC50 values of 0.83 nM and 203.1 nM, respectively. The induced degradation of EGFR by this compound is associated with autophagy [1].

PROTAC EGFR degrader 6 is a potent PROTAC EGFR degrader that effectively reduces EGFR Del19 levels in HCC827 cells, exhibiting a DC50 of 45.2 nM. It notably promotes apoptosis and induces G1 phase arrest in HCC827 cells [1].

PROTAC EGFR Degrader 3, a highly potent molecule, exhibits remarkable cellular activity against H1975 and HCC827 cells, maintaining high selectivity. It additionally reveals the lysosome's crucial role in the degradation mechanism of mutant EGFR [1].

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/HER2/DHFR-IN-2 (Compound 4b) serves as an inhibitor for EGFR, HER2, and DHFR, with IC50 values of 0.248, 0.156, and 0.138 μM, respectively. It exhibits anticancer activity, displaying IC50 values of 9.14, 7.33, 14.18, 24.87, 20.07, and 6.16 μM in Hep G2, HeLa, HEp-2, HCT 116, PC-3, and MCF7 cancer cell lines, respectively. Additionally, EGFR/HER2/DHFR-IN-2 has been shown to reduce the growth of breast cancer tumors [1].

PROTAC EGFR degrader 2 is a potent compound with exceptional antiproliferative activity, evidenced by its IC50 of 4.0 nM, and exhibits strong EGFR degradation activity with a DC50 of 36.51 nM. It is suitable for synthesizing nitroreductase (NTR)-responsive PROTACs [1].

EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.092 μM for HER2, respectively. Moreover, it demonstrates inhibition of DHFR with an IC50 of 0.193 μM. Notably, this compound induces cell cycle arrest in the S phase and triggers apoptosis in MCF7 breast cancer cells [1].

PROTAC EGFR degrader 7 (compound 13b) is a potent, selective, CRBN-recruiting EGFRL858R/T790M degrader with a DC50 of 13.2 nM. It effectively inhibits proliferation of NCI-H1975 cells with an IC50 of 46.82 nM, induces apoptosis, and causes a G2/M phase arrest in these cells. Demonstrating antitumor activity, this compound is applicable in non-small cell lung cancer (NSCLC) research.

PROTAC EGFR degrader 7 (compound 13b) is a potent, selective CRBN-recruiting agent targeting EGFR L858R/T790M mutations with a DC50 of 13.2 nM. It effectively inhibits proliferation in NCI–H1975 cells with an IC50 of 46.82 nM and significantly triggers apoptosis and G2/M phase arrest in these cells. Demonstrating antitumor efficacy, PROTAC EGFR degrader 7 holds promise for non-small cell lung cancer (NSCLC) research [1].

[pTyr5] EGFR (988-993) is a compound obtained from the auto-phosphorylation site, Tyr992, located within the sequence of the epidermal growth factor receptor (EGFR 988-993). This compound is frequently found bound with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B).

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-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-68 (Compound 8d) is a highly effective EGFR inhibitor, demonstrated by its potent inhibition activity with an IC50 value of 0.33 μM. It exhibits notable anticancer properties [1].

EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor targeting EGFR and CDK-2, demonstrating IC50 values of 89.6 nM for EGFR and 165.4 nM for CDK-2. It prompts apoptosis in MCF-7 cells and causes S phase cell cycle arrest, exhibiting substantial anti-cancer activity with an IC50 of 2.74 μM against MCF-7 cells [1].

EGFR-IN-33, an acrylamide derivative, is a low-toxicity antitumor agent and a potent inhibitor of EGFR. Among others, overexpression and mutation of the epidermal growth factor receptor (EGFR) has been shown to lead to uncontrolled cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-33 exhibits potential for the study of EGFR mutation-related diseases.

EGFR/HER2-IN-5 is an irreversible, orally active dual inhibitor of EGFR activity (IC50: 0.6 nM). EGFR/HER2-IN-4 shows potent EGFR kinase inhibitory activity against L858R and T790M mutations. EGFR/HER2-IN-4 exhibits significant anti-tumour effects in vivo and can be used to study lung cancer.

EGFR-IN-38 is a low-toxicity, acrylamide derivative antitumor agent that is a potent inhibitor of EGFR. Among others, overexpression and mutation of the epidermal growth factor receptor (EGFR) has been shown to lead to uncontrolled cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-38 exhibits potential for research in EGFR mutation-related diseases.

EGFR-IN-58 is a potent, selective, ATP-competitive inhibitor of EGFR. EGFR-IN-58 exhibits significant cytotoxicity against melanoma, colon and blood cancers.

EGFR-IN-39, an acrylamide derivative, is a potent inhibitor of EGFR. EGFR-IN-39 is an antitumor agent with low toxicity and side effects. Among them, the overexpression and mutation of epidermal growth factor receptor (EGFR) have been clearly confirmed to cause uncontrollable cell growth, and are related to the progression of most cancer diseases, especially NSCLC. EGFR-IN-33 has the potential to study EGFR mutation-related diseases.

EGFR-IN-50 is a potent EGFR inhibitor targeting L858R resistance mutations, acting on TEL-EGFR-L858R-BaF3 and TEL-EGFR-T790M-L858R-BaF3 with GI50 values of 8 nM and 6.03 μM, respectively. EGFR-IN-50 exhibits anti-proliferative effects on cancer cells. .

EGFR-IN-46 is a potent dual inhibitor of EGFR (IC50: 20.17 nM) and FAK (IC50: 14.25 nM) that significantly inhibits the growth of cancer cells and induces apoptosis.

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-56 (Compound 13a) is a potent inhibitor of EGFR, acting on EGFRT790M (IC50: 541.7 nM) and EGFRT790M/L858R (IC50: 132.1 nM). EGFR-IN-56 blocks the cell cycle of cancer cells in the G2/M phase and induces EGFR-IN-56 blocks the G2/M phase of the cancer cell cycle and induces apoptosis.

EGFR-IN-542 is a novel EGFR inhibitor. EGFR-IN-542 significantly reduces myocardial inflammation, fibrosis, apoptosis and dysfunction. It shows promise for use in the treatment of obesity-induced cardiac complications.

EGFR-IN-44 is a potent, orally active inhibitor of EGFRtyrosine kinase (IC50: 4.11 nM). EGFR-IN-44 has an oral bioavailability of 33.57% and induces apoptosis. EGFR-IN-44 can be used to study non-small cell lung cancer.

EGFR-IN-78 (compound A5), a 2-aminopyrimidine derivative, serves as a reversible EGFR C797S-TK inhibitor and an apoptosis inducer. It exhibits anti-proliferative properties, impedes EGFR phosphorylation, and induces G2/M phase cell cycle arrest [1].

Mutant EGFR inhibitor is a selective and potent Mutated EGFR inhibitor, inhibits L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant.

EGFR-IN-8, a dual inhibitor targeting both EGFR and c-Met, shows potential as a promising candidate for further development in treating EGFR TKI-resistant NSCLC.

EGFR peptide (myristoylated), a synthetic peptide inhibitor of PKC (IC50 = 5 µM), corresponds to the intracellular region's amino acid sequence of EGFR. It effectively reverses doxorubicin resistance in UV-2237M (UV-2237M-ADRR) fibrosarcoma cells at a concentration of 1 µM.

E07 Aptamer, targeting the human epidermal growth factor receptor (hEGFR), competes with epidermal growth factor (EGF) for binding to a unique epitope on EGFR. This aptamer not only binds to EGFR-expressing cells but also inhibits receptor autophosphorylation and thwarts tumor cell proliferation in three-dimensional matrices, positioning it as a useful tool for tumor disease research [1].

EGFR-IN-83 (Compound 9), an EGFR inhibitor with an IC50 of 2.53 nM, exhibits antiproliferative effects on MCF-7 and MDA-MB-231 cell lines, with respective IC50 values of 2.50 μM and 1.96 μM. Furthermore, EGFR-IN-83 is capable of inducing cell apoptosis [1].

ALK/EGFR-IN-2 is a potent dual inhibitor targeting ALK and EGFR, promoting apoptosis and G0/G1 cell cycle arrest in cancer cells. It effectively suppresses proliferation in H1975, PC9, and Baf3-EML4-ALK cancer cell lines, demonstrating IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively [1].

EGFR/CDK2-IN-2 (compound 6a) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 19.6 nM and 87.9 nM, respectively. It promotes apoptosis in MCF-7 cells and halts cell cycle progression during the S phase. Additionally, this compound demonstrates notable anticancer activity, inhibiting MCF-7 cells with an IC50 of 0.39 μM [1].

EGFR-IN-79 (compound 21), an EGFR inhibitor, exhibits antitumor activity through ROS-independent apoptosis and EGFR/AKT/mTOR-mediated autophagy. It effectively induces cell death in proliferating and quiescent zones of EJ28 spheroids and demonstrates a safety profile in zebrafish-based models [1].

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-IN-36 is a potent inhibitor of EGFR, capable of acting on EGFR (WT) (IC50: 19.09 nM), HER2 (WT) (IC50: 120.01 nM), HER2 (A775_G776insYVMA) (IC50: 2.35 nM). EGFR-IN-36 exhibits the potential to study wild and/or mutant EGFR and/or HER2 kinase-mediated tumors.

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/BRAF-IN-1, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent inhibitor of EGFR/BRAF, inhibiting BRAFV600E (IC50:45 nM) and cancer cell proliferation (GI50=35 nM), with good antioxidant effect.

EGFR-IN-30, a potent inhibitor of EGFR, exhibits IC50 values of 1-10 nM and <1 nM for EGFR (WT) and EGFR (L858R/T790M/C797S), respectively. This compound is of potential interest for research into diseases characterized by cell proliferation, such as cancer.

EGFR/BRAFV600E-IN-1 (Compound 23) is a potent dual inhibitor of EGFR (IC50: 0.08 μM) and BRAFV600E (IC50: 0.15 μM). EGFR/BRAFV600E-IN-1 exhibited anti-proliferative effects on A-549 (IC50: 1.2 μM), MCF-7 (IC50: 0.79 μM), Panc-1 (IC50: 1.3 μM), HT-29 (IC50: 1.23 μM).