erbb 2

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

ErbB-2-binding peptide (HER2-binding peptide), a tumor-targeting peptide, holds potential for cancer research applications [1].

EGFR/ErbB-2/ErbB-4 inhibitor-2 (EGFR/ErbB2 Inhibitor) is a cell-permeable inhibitor of EGFR and c-ErbB2 (IC50s = 20 and 79 nM, respectively)

Butein (2’,3,4,4’-tetrahydroxy Chalcone), a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit EGFR.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively).

SU5204 (3-[(2-Ethoxyphenyl)methylidene]-1H-indol-2-one), an analogue of SU5025, pharmacologically inhibits VEGFR2(IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2)

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

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

2'-Thioadenosine (PD157432) serves as a selective and irreversible inhibitor of ErbB-1 and ErbB-2 tyrosine kinases, demonstrating an IC50 value of 45 µM against ErbB-2. It achieves covalent inactivation of ErbB-1 through modification of a cysteine residue within the enzyme's active site [1].

Lapatinib tosylate (GW572016), a robust and orally administered inhibitor specifically targeting the tyrosine kinase domains of ErbB-2 and EGFR, exhibits inhibitory concentration 50 (IC50) values of 10.2 nM and 9.8 nM against purified EGFR and ErbB-2, respectively.

(S)-Sunvozertinib (DZD9008) is a rationally designed selective, irreversible EGFR/HER2 inhibitor.