EGFR

CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase with IC50 values of 5.3 nM for drug-resistant mutant EGFR T790M and 8.3 nM for WT EGFR kinases.

EGFR-IN-2 is a non-covalent, orally available and mutation-selective EGFR inhibitor for the treatment of non-small cell lung cancer (NSCLC), with high selectivity for resistant single and double mutant T790M with IC50 = 27 nm to 33 nM, and low inhibitory activity for wild-type H292 (IC50 = 218 nM).

EGFR/ErbB-2/ErbB-4 inhibitor-2 (EGFR/ErbB2 Inhibitor) is a cell-permeable compound that inhibits EGFR and c-ErbB2 with IC50 values of 20 nM and 79 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-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-IN-7 (TQB3804) is a selective and potent EGFR kinase inhibitor.

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.

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-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-12 (EGFR Inhibitor) is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells.

EGFR-IN-76 is a potent EGFR inhibitor.

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-16 (AG473) is an inhibitor of EGFR in human A431 cells.

Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) and a HER2-targeted cytotoxic agent, consisting of an anti-HER2 monoclonal antibody conjugated to MMAE via a cleavable linker, used for the treatment of HER2-expressing solid tumors including gastric cancer, breast cancer, and urothelial carcinoma.

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.

Pertuzumab (anti-HER2) a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors impairs the ability of HER2 to bind to other members of the HER family.

Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

Rezivertinib (BPI-7711) is an orally available, selective and potent inhibitor of tyrosine kinase (EGFR) with antitumor activity for central nervous system disorders.

NSC 228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulating EGFR tyrosine phosphorylation.

Tesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor with IC50 values ​​of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4.