EGFR

EGFR-IN-85 (Compound 1), an EGFR inhibitor, exhibits potent activity with an IC50 of 0.19 μM against EGFRvⅢ phosphorylation and can suppress intratumoral EGFR

EGFR-IN-61 inhibits EGFR kinase (IC50: 42 nM L858R/T790M, 137 nM L858R/T790M/C797S, 743 nM WT) and slows A549 & H1975 cell growth (IC50: 2.14 & 1.82 μM).

BGB-102 (JNJ-26483327) is a kinase inhibitor targeting FLT3 and YES1 and an antagonist targeting EGFR and VEGFR3.

EGFR-IN-33, a low-toxicity acrylamide, inhibits EGFR, aiding against cancer, especially NSCLC (from WO2021185348A1, comp. 13).

EGFR-IN-87 is an EGFR tyrosine kinase inhibitor with potent inhibitory activity, exhibiting IC50 values of 3.1 nM, 1.3 nM, and 7.1 nM against EGFR_d746-750,

Sevabertinib (BAY 2927088) is an EGFR tyrosine kinase inhibitor, with anticancer activity, used in research on non-small cell lung cancer.

EGFR-IN-1 HCl targets L858R/T790M EGFR mutants over wild-type; IC50: 4 nM in H1975, 28 nM in mutant HCC827 cells.

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

HER2-IN-8 is an inhibitor of HER-2 that can be used in the study of cancer and inflammation-related diseases.

JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active inhibitor of EGFR with an IC 50 of 15 nM for EGFR L858R/T790M [1].

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.

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.

Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR/HER2.

HER2-IN-9, an oral HER2 inhibitor (IC50: 0.03 μM), hinders growth and spread of HER2+ breast cancer.

BML-265 is a potent inhibitor of EGFR tyrosine kinase (EGFR tyrosine kinase). It disrupts Golgi apparatus integrity in human cells and hinders the transport of secretory proteins across various substances. In contrast, BML-265 does not affect the integrity and transport of the Golgi apparatus in rodent cells.

PROTACHer3-binding moiety 2 is an inhibitor of Her3. It is applicable in the synthesis of PROTACHer3 Degrader-8.

Tyrosine Protein Kinase Substrate is a polypeptide molecule with the sequence RRLIEDNEYTARG.

EGFR-IN-48: potent EGFR inhibitor, oral, IC50: 0.193-66.7 nM, blocks EGFR mutants & BaF3/PC-9 cell proliferation.

JBJ-09-063: EGFR inhibitor, IC50s 0.147-0.396 nM for various mutants; hinders EGFR/Akt/ERK1/2 phosphorylation; targets TKI-sensitive/resistant lung cancer.

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

EGFR/HER2-IN-5: Irreversible, oral dual EGFR inhibitor, IC50 0.6 nM, targets L858R/T790M mutations, anti-tumor in vivo for lung cancer study.

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

D-69491 hydrochloride is an inhibitor of HER-2 tyrosine kinase activity, blocking the phosphorylation of HER-2 and inhibiting the proliferation of SKOV-3 cells. It exhibits antitumor activity.

HER2-IN-7 is a potent HER2 inhibitor with potential for researching ErbB-related diseases, especially cancer.

EGFR-IN-159 (compound 12) is a dihydropyrimidine and a potent EGFR inhibitor with an IC50 of 29.00 nM. It exhibits dose-dependent inhibition of EGFR and HER2. The compound shows cytotoxicity against MCF-7 breast cancer cells and Vero cells with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. EGFR-IN-159 does not cross the blood-brain barrier (BBB) and demonstrates significant anticancer activity.

EGFR/BRAF-IN-1 inhibits EGFR/BRAF (BRAFV600E IC50: 45 nM, GI50: 35 nM) and has antioxidant properties.

NSC381467: Potent, oral EGFR-TK inhibitor with strong antiproliferative effects, promising for cancer research.

EGFR-IN-18 strongly inhibits L858R/T790M/C797S mutant EGFR (4.9 nM) and also targets wild-type EGFR (47 nM).

Potent EGFR/HER2/DHFR inhibitor for MCF-7 breast cancer; IC50: 0.153/0.108/0.291 μM; arrests G1/S phase, triggers apoptosis.

Andamertinib is an EGFR inhibitor with antitumor activity.

EGFR-IN-17: potent, selective EGFR inhibitor, IC50 of 0.2 nM, overcomes C797S drug resistance.

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).

Sacibertinib inhibits Trk, targeting EGFR-TK (EC50 110 nM) & HER2 (EC50 244 nM), with anticancer properties.

EGFR-IN-34 is a low-toxicity, acrylamide derivative antitumor agent that is a potent inhibitor of EGFR.

EGFRLigand-Linker Conjugates 1 is a Target Protein Ligand-Linker Conjugate comprising an EGFR ligand and a PROTAC linker, designed to recruit the E3 ligase. It is used in the synthesis of PROTACEGFRdegrader 3.

Neptinib (NEP010), a derivative of Afatinib, exhibits enhanced antitumor properties and improved pharmacokinetics when administered orally. It demonstrates a notable suppression of tumor expansion in mouse models of non-small cell lung cancer harboring various EGFR mutations. Furthermore, Neptinib effectively inhibits the EGFR kinase family, exhibiting IC 50 values of 0.24 nM for EGFR wt, 7.25 nM for EGFR L858R/T790M, 0.46 nM for EGFR L858R, and 1.79 nM for EGFR T790M.

EGFR-IN-35, an acrylamide-based EGFR inhibitor, shows promise for EGFR mutation-related cancers like NSCLC.

EGFR-IN-38: low-toxic acrylamide-derived EGFR inhibitor, targets NSCLC, patented for research on EGFR mutation-related diseases.

HER2-IN-21 (compound 657994) is an inhibitor of the human epidermal growth factor receptor 2 (HER2) with an IC50 value of 3.85 μM.

EGFR-IN-160 is an EGFR inhibitor with IC50 values of 1.62, 0.49, and 0.98 μM for EGFRWT, EGFRT790M, and EGFRL858R/T790M/C797S, respectively. It can induce cell cycle arrest at the G2/M and S phases and apoptosis (Apoptosis) in NCI-H522 cells, demonstrating anticancer properties. Additionally, EGFR-IN-160 exhibits antioxidant activity against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM).

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

SORT1-IN-5 (compound 3) is a SORT1 inhibitor capable of crossing the blood-brain barrier. The MSOH salt form of SORT1-IN-5 exhibits a certain degree of oral bioavailability.

Si306, an Src inhibitor, exhibits antitumor activity by reducing the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), thereby inhibiting the invasion of human glioblastoma (GBM).

EG31 is an EGFR inhibitor that effectively suppresses the proliferation of triple-negative breast cancer (TNBC) cells by inhibiting the EGFR signaling pathway. It demonstrates a GI50 value of 498.90 nM for MDA-MB-231 cells and 740.73 nM for Hs578T cells, while also inducing apoptosis. Additionally, EG31 retains its antiproliferative activity against 5-fluorouracil (5-FU) resistant TNBC cells, with a GI50 of 519.5 nM. EG31 is applicable in research on TNBC resistance.

BPI-15086 is an orally active, effective, irreversible inhibitor selective for mutations, targeting both EGFR and the T790M resistance mutation tyrosine kinase. It can be utilized in the study of non-small cell lung cancer.

ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.

EGFR/HER2-IN-8 inhibits EGFR, HER2, DHFR (IC50: 0.45, 0.244, 5.669 μM); useful in cancer research, safe and selective.