egfr-inhibitor-451

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

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 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-451 is an EGFR inhibitor, attenuating Ang II-induced Kidney Fibrosis.

EGFR Kinase Inhibitor 4 (Compound 4) acts as a bivalent ATP-allosteric inhibitor targeting EGFR, with a potent inhibitory effect (IC 50: 1.8 nM) on mutant EGFR (LRTMCS). It is primarily utilized in the study of non-small cell lung cancer (NSCLC) [1].

EGFR kinase inhibitor 1 is a potent inhibitor of EGFR that acts on WT (IC50: 37 nM), l885R T790M (IC50: 1.7 nM), and L858R T790M C797S (IC50>300 nM). It is capable of blocking the cell cycle in G0 G1 phase, inducing apoptosis, and has an inhibitory effect on cell metastasis. Additionally, EGFR kinase inhibitor 1 exhibits anti-proliferative and anti-tumor effects.

EGFR kinase inhibitor 3 (compound 2) serves as a dual-action inhibitor targeting both ATP and allosteric sites of the EGFR kinase, exhibiting potent IC50 values of less than 10 nM for wild-type EGFR, 1.5 nM for the L858R mutation, 0.059 nM for the L858R T790M mutation, and 0.064 nM for the L858R T790M C797S mutation. It is classified as a C-linked inhibitor [1].

Pebezertinib (BLU 451) is an orally effective inhibitor of EGFR, capable of penetrating the central nervous system (CNS). It is utilized in research targeting non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertions.

EGIS-8332 is a potent and selective non-competitive AMPA receptor antagonist. EGIS-8332 inhibits AMPA/kainate ion channels and cell death. EGIS-8332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA- and quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons (IC(50)=5.1-9.0 microM), in vitro. EGIS-8332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimental disease models, and on its low side effect potential.