ErbB3/HER3 Inhibitor

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.

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.

TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC₅₀ of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.

Lumretuzumab (Anti-Human ERBB3 Recombinant Antibody) is a humanized anti-HER3 (ERBB3) monoclonal antibody. Lumretuzumab effectively inhibits the activity of key oncogenic signaling pathways such as PI3K/AKT and MAPK. Lumretuzumab has been optimized through glycosyl engineering to enhance antibody-dependent cell-mediated cytotoxicity (ADCC). Lumretuzumab can be used to study HER3-positive, HER2-low-expressing solid tumors, especially breast cancer.

SIBP-03 is a specifical anti-HER3 antibody. SIBP-03 binds strongly and specifically to recombinant HER3 protein. SIBP-03 inhibits HER3 activation, as well as the downstream PI3K/AKT signaling pathway. SIBP-03 exhibits anticancer activity against squamous cell carcinoma, non-small cell lung cancer, gastric cancer, and breast cancer. SIBP-03 synergistically enhances the antitumor activity of DS-8201 (HY-138298A) and Cetuximab (HY-P9905).

PD158780 is a potent EGFR family inhibitor with IC₅₀s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.

Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody targeting EGFR. Duligotuzumab blocks the binding of ligands to these two receptors, inhibits downstream HER/ErbB, AKT and MAPK signaling pathways, induces antibody-dependent cellular cytotoxicity, reduces the proliferation and migration abilities of cancer cells, promotes apoptosis, exerts radiosensitizing effects, and reverses EGFR resistance in cancer cells. Duligotuzumab can be used in tumor-related research.

Sec61-IN-3 is a Sec61 inhibitor. Sec61-IN-3 shows a significant inhibitory effect on PD-1 related reporter gene cell models (PD1tsGluc) (IC₅₀ = 42 nM), and also has certain inhibitory activity on Her3 (IC₅₀ = 99 nM), IL2 (IC₅₀ = 144 nM) related reporter pathways, but has a relatively weak inhibitory effect on the TNFα (IC₅₀ = 580 nM) pathway. Sec61-IN-3 can be used for cancer research.

CDX-3379 is a humanized monoclonal antibody inhibitor targeting ErbB3. CDX-3379 binds to ErbB3, blocking the dimerization of ErbB3 with other receptors, thereby inhibiting the phosphorylation of ErbB3. CDX-3379 can inhibit the growth and proliferation of tumor cells. CDX-3379 is promising for research of tumors expressing ErbB3 and NRG1, such as HNSCC.

Afatinib (BIBW 2992) oxalate 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 oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

TX2-121-1 is a potent and selective Her3 (ErbB3) degrader that contains a hydrophobic adamantane moiety. TX2-121-1 has an IC₅₀ of 49 nM for Her3. TX2-121-1 inhibits Her3-dependent signaling and heterodimerization of Her3. TX2-121-1 has the ability to inhibit cell proliferation. TX2-121-1 can be used in the study of tumors. (Pink: Her3 inhibitor (HY-164988); Black: Linker; Blue: Adamantane (HY-N2427)).

MP-RM-1 is an antibody-based, non-competitive ErbB-3 inhibitor with a K_d value of 32.7 nM. MP-RM-1 inhibits both ligand-dependent and ligand-independent ErbB-3 activation, blocks ErbB-2/ErbB-3 heterodimerization, induces ErbB-3 internalization and degradation, and suppresses the phosphorylation of downstream Akt. MP-RM-1 exerts its antagonistic effect through a non-competitive mechanism. MP-RM-1 inhibits tumor growth in melanoma and prostate cancer xenograft models in nude mice and reduces the proliferative activity of tumor cells.

Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) is an anti-mouse E-Cadherin/CD324 IgG1 monoclonal antibody. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can downregulate the HER signaling axis and PI3K/Akt/mTOR signaling pathway. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can inhibit the proliferation of tumor cells and induce their apoptosis. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can be used for researches on cancer and inflammation conditions such as breast cancer, chronic compression injury (CCI) and asthma.

PROTAC Her3-binding moiety 2 is a Her3 inhibitor. PROTAC Her3-binding moiety 2 can be used for synthesis of PROTAC Her3 Degrader-8 (HY-153796).