erbb2

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 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, shows significant potential for cancer research applications [1].

Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4).

Dacomitinib (PF299)(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.

Lapatinib Ditosylate (Tykerb ditosylate) is an effective EGFR and ErbB2 inhibitor (IC50: 10.8/9.2 nM for EGFR/ErbB2).

Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2/10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.

Tucatinib (ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).

Lapatinib ditosylate (Lapatinib tosilate) monohydrate is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib ditosylate monohydrate therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.

AZD8931 is a reversible and ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 (IC50 of 4 nM, 3 nM and 4 nM, respectively).

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.

dual EGFR/ErbB2 tyrosine kinase inhibitor

AG490 (Tyrphostin B42) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn, Lck, Syk, Btk, and Src.

Mubritinib (TAK-165) (TAK-165) is a potent inhibitor of HER2 ErbB2 with IC50 of 6 nM.

Pelitinib (EKB-569) (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).

Sapitinib (AZD-8931) , a reversible, ATP competitive inhibitor of EGFR(IC50=4 nM), ErbB2(IC50=3 nM) and ErbB3(IC50=4 nM), is more effective over Gefitinib or Lapatinib against NSCLC cell, 100-fold more specific for the ErbB family over MNK1 and Flt.

Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK) with an IC50 of 1.3 nM.

Tyrphostin AG 528 (Tyrphostin B66) is an inhibitor of EGFR (IC50: 4.9 μM) and ErbB2 (IC50: 2.1 μM).

AEE788 (NVP-AEE 788) has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.

AG-494 (Tyrphostin B48) is an inhibitor of epidermal growth factor receptor kinase.

CP-724714 (CP724714) is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), >640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc.

Tyrphostin AG 879 (AG 879) effectively inhibits HER2 ErbB2 with an IC50 of 1 μM, demonstrating 100- and 500-fold higher selectivity for ErbB2 over EGFR and PDGFR, respectively.

Allitinib tosylate (AST-1306) is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, respectively.

WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).

Canertinib dihydrochloride (PD-183805 dihydrochloride) is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities.

PD 158780 reversibly inhibits auto and transphosphorylation of all four members of the ErbB receptor superfamily: EGFR, ErbB2, ErbB3, and ErbB4 (IC50s: 8μM, 49 nM, 52 nM, and 52 nM in cell assay).

Allitinib (AST-1306) (AST-1306) has anti-cancer activity，and it is an irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. [1]

ErbB receptor family inhibitor

HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM), effectively suppressing EGFR autophosphorylation (at Y1068), as well as AKT and MAPK phosphorylation.

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

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].

BI-1622 is a highly selective, orally active HER2(ERBB2) inhibitor (IC50: 7 nM). BI-1622 is >25-fold selective for EGFR. In a mouse model of transplanted tumors transfected with H2170 and PC9 cells, BI-1622 exhibited high in vivo antitumor effects with good drug metabolism and pharmacokinetic properties.

Varlitinib Tosylate is a selective and potent inhibitor of ErbB1(EGFR) and ErbB2(HER2).

AV-412 (MP412) is an EGFR inhibitor for EGFR, EGFR T790M, EGFR L858R, EGFR L858R T790M, and ErbB2, with IC50 values of 0.75, 0.79, 0.5, 2.3, and 19 nM, respectively.

CP-654577 is a selective p185(ErBB2) kinase inhibitor that reduces the level of the activated form of mitogen-activated protein kinase in SKBR3 human breast cancer cells.

Lapatinib-d4 is a deuterated compound of Lapatinib. Lapatinib has a CAS number of 231277-92-2. Lapatinib is a dual inhibitor of Lapatinib is a dual ErbB2/EGFR (IC50: 9.2/10.8 nM) inhibitor

AV-412 free base is an EGFR inhibitor (IC50s: 0.75, 0.79, 0.5, 2.3, 19 nM for EGFR, EGFR(T790M), EGFR(L858R), EGFR(L858R T790M) and ErbB2).

PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.

Timigutuzumab (GEXMab73) is a humanized monoclonal antibody targeting ErbB2, with potential application in cancer research [1].

Imbotolimod, a humanized monoclonal antibody of the immunoglobulin G1-kappa class, exhibits both anti-ERBB2 and antineoplastic activities. It is a derivative of telratolimod [1].

AG-825（Tyrphostin C15） is a selective and competitive ErbB2 inhibitor that inhibits tyrosine phosphorylation with an IC50 value of 0.35 μM.AG-825 (Tyrphostin C15) inhibits HER2 and shows anticancer activity in a mouse xenograft model of breast cancer.AG-825 ( Tyrphostin C15) is a potentially active molecule for overcoming manganese-induced neurotoxicity or the development of Alzheimer's disease, and promotes apoptosis in human neutrophils, which could be used in the study of breast cancer.

GI261520A is a potent egfr/erbb2 dual inhibitor

Selatinib is an orally active and potent dual inhibitor of EGFR and ErbB2 with anticancer activity that inhibits the growth of NCI-N87 tumor cells.

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

H2-Gamendazole is a novel compound for spermatogenesis inhibition and cancer therapy as an inhibitor of heat shock proteins and or elongation factor 1 alpha, and is an Hsp90 regulator.

Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors, has potent antitumor activities.

HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.

Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50 values of 7 nM for HER1, 2 nM for HER2, and 4 nM for HER4.

(E/Z)-CP-724714, comprising racemic mixtures of (E)-CP-724714 and (Z)-CP-724714 isomers, is a potent, selective, and orally active inhibitor of ErbB2 (HER2)[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.

Dantrolene sodium (Lapatinib ditosylate monohydrate) salt is a skeletal muscle relaxant and can interfere with excitation-contraction coupling in the muscle fiber. It is used for the treatment of spasticity and other neuromuscular abnormalities. Its mechanism of action is may not central, but dantrolene is usually grouped with the central muscle relaxants.