ErbB2/HER2 Inhibitor

Trastuzumab is a humanized IgG1 monoclonal antibody that selectively binds to HER2 with high affinity. Trastuzumab can be used for the research of HER2-positive metastatic breast cancer and gastric cancer. (Note: The product specifications below only indicate the effective content of Trastuzumab. The component ratio of this product is Trastuzumab : excipients = 1:0.6-1:0.9.)

Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.

Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC₅₀ of 8 nM.

Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC₅₀s of 59 nM and 92 nM, respectively.

Disitamab vedotin (RC48) is a HER2-targeted antibody-drug conjugate (ADC), formed by conjugation of the humanized anti-HER2 antibody Disitamab (HY-P99854) with drug-linker VcMMAE (HY-15575). VcMMAE consists of a cleavable MC-Val-Cit-PAB linker and the microtubule inhibitor MMAE (HY-15162). After binding to HER2 and undergoing endocytosis, Disitamab vedotin releases MMAE in lysosomes, which further inhibits microtubule assembly, arrests mitosis and induces apoptosis, while also exerting a bystander effect. Disitamab vedotin can be used in studies of HER2-positive breast cancer.

Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC₅₀s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice.

Pertuzumab, a humanized IgG1 monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.

Zanidatamab (ZW25) is a humanised, bispecific monoclonal antibody targeting 2 distinct HER2 epitopes (ECD2 and ECD4). Zanidatamab has anti-tumour activity.

Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.

Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC₅₀s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC₅₀s of 13 and 38 nM, respectively.

Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC₅₀s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52).

CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC₅₀s of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC₅₀ of 6 nM.

Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research.

Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC₅₀s of 59 nM and 92 nM, respectively.

Disitamab (RC48-0) is a humanized monoclonal antibody targeting HER2. Disitamab can be used in the synthesis of antibody-drug conjugates (ADCs), Disitamab vedotin (HY-P9985).

Lapatinib ditosylate (GW572016 ditosylate) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.