EGFR Inhibitor

Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC₅₀s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC₅₀ of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity.

EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC₅₀s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR^L858R, EGFR^T790M and EGFR^L858R/T790M at 10 μM ATP, respectively.

Anbenitamab (KN-026) is a bispecific antibody simultaneously targeting extracellular domains II and IV of human HER2. Anbenitamab blocks both ligand-dependent and ligand-independent HER2 signaling pathways. Anbenitamab mediates antibody-dependent cellular cytotoxicity (ADCC) via FcγIIIa binding. Ambrinitumab can be used in research for lung cancer, HER2-positive metastatic breast cancer (MBC), gastric cancer, and gastroesophageal junction cancer.

Tubeimoside II is an orally active triterpenoid saponin and antiviral agent that binds to PACT/PRKRA with K_d values of 5.37 μM and 133.1 μM, respectively. Tubeimoside II inhibits oxidase-dependent EGFR activation and reduces TGF-β1-induced oxidative stress. Tubeimoside II activates the RIG-I signaling pathway and increases IFN-β secretion. Tubeimoside II suppresses TPA-induced ear edema, mouse sarcoma 180 growth, and TPA-induced skin tumor formation. Tubeimoside II exerts broad-spectrum antiviral activity against SARS-CoV-2, HCoV-OC43, and IAV-H1N1/FM1. Tubeimoside II can be used in research related to retinoblastoma, respiratory viral infections, skin tumors, and sarcoma 180.

Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC₅₀ of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC₅₀=3.4 μM) and a range of other related tyrosine kinases (IC₅₀>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.

PF-06672131 is an alkynylated afatinib derivative and a small molecule probe that is reactive to cysteine. PF-06672131 is an inhibitor of epidermal growth factor receptor (EGFR) kinase that targets the ATP pockets of EGFR. PF-06672131 can be used for activity-based protein profiling studies.

Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC₅₀s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice.

STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations.

TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC₅₀ of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).

Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC₅₀ of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC₅₀ of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity.

Depatuxizumab MMAE is an antibody-drug conjugate (ADC) comprising an anti EGFR monoclonal antibody (Depatuxizumab) (HY-P99849) and the cytotoxic agent Monomethyl auristatin E (MMAE) (HY-15162). Depatuxizumab MMAE can be used for the study of EGFR-expressing advanced solid tumors.

Broussoflavonol F is a potent dual inhibitor of the HER2-RAS-MEK-ERK signaling pathway and mushroom tyrosinase with an IC₅₀ value of 82.3 μM. Broussoflavonol F downregulates the expression of RAS, HER2, phosphorylated BRAF, phosphorylated MEK and phosphorylated Erk proteins. Broussoflavonol F induces cell cycle arrest and apoptosis, and exhibits cytotoxicity in colon cancer cells. Broussoflavonol F inhibits endothelial proliferation, migration and tube formation, suppresses subintestinal vascular development, and reduces the mRNA levels of angiogenesis-associated genes.Broussoflavonol F can be used for colon cancer research.

HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC₅₀s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.

AFM24 is a bispecific antibody with a TandAb structure expressed in CHO, targeting EGFR&Fc-gamma-RIIIA. AFM24 contains a huIgG1-SCFV heavy chain and a λ light chain, with a predicted molecular weight (MW) of 196.34 kDa. The isotype control for AFM24 can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.

Bafisontamab (EMB-01) is a bispecific antibody targeting EGFR and cMET with antitumor activity.

AZ7550 Mesylate is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.

Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC₅₀ of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis.

Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR^L858R, EGFR^L858R/T790M, EGFR^T790M and EGFR^L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Imgatuzumab (RG 7160) is a humanized monoclonal antibody against the EGFR. Imgatuzumab acts as an immunomodulator. Imgatuzumab can be used in research of cancer.