ErbB2/HER2
The ErbB2/HER2 receptor is a member of the ErbB receptor tyrosine kinase family, lacking a direct ligand yet serving as a critical dimerization partner for other ErbB receptors[1][2]. Mechanistically, HER2 homodimers and heterodimers activate multiple downstream pathways including PI3K/Akt, MAPK/ERK, and NF-κB signaling, influencing cell proliferation, survival, and transcriptional regulation[3][2][4]. Compared with related isoforms such as HER3, which requires ligand binding for activation, HER2’s constitutive activity confers robust signaling capacity and amplifies oncogenic potential[1][5][4]. In disease models, HER2 overexpression is observed in 15-20% of breast cancers and in experimental prolactinoma, driving hormone secretion and cellular proliferation[6][7][8]. The receptor also interacts with calmodulin, which modulates its phosphorylation and downstream kinase activity, linking calcium signaling to HER2-mediated pathways[6]. Experimental inhibitors such as trastuzumab, pertuzumab, lapatinib, and AZD8931 selectively target HER2-containing dimers, modulating receptor activation and sensitizing cancer cells to chemotherapy[9][2][4]. The distinct signaling patterns induced by HER2 homodimers versus HER2-containing heterodimers influence therapeutic responses, with Akt activation levels correlating with drug resistance[2][4]. Collectively, HER2 functions as a signaling hub, with isoform-specific interactions and pharmacologic modulation providing a platform for both mechanistic and translational research[1][2].
References:
- [1]. Khalili M, et al. Underserved Does Not Mean Undeserved: Unfurling the HCV Care in the Safety Net. Dig Dis Sci. 2018 Dec;63(12):3250-3252. [Content Brief]
- [2]. Ali SR, et al. Nerve Density and Neuronal Biomarkers in Cancer. Cancers (Basel). 2022 Oct 1;14(19):4817. [Content Brief]
- [3]. Kurokawa H, et al. ErbB (HER) receptors can abrogate antiestrogen action in human breast cancer by multiple signaling mechanisms. Clin Cancer Res. 2003;9(1 Pt 2):511S-515S. [Content Brief]
- [4]. Zhang Y, et al. HER/ErbB receptor interactions and signaling patterns in human mammary epithelial cells. BMC Cell Biol. 2009;10:78.
- [5]. Li H, et al. The ErbB2/Neu/HER2 receptor is a new calmodulin-binding protein. Biochem J. 2004 Jul 1;381(Pt 1):257-66. [Content Brief]
- [6]. Fukuoka H, et al. HER2/ErbB2 receptor signaling in rat and human prolactinoma cells: strategy for targeted prolactinoma therapy. Mol Endocrinol. 2011 Jan;25(1):92-103. [Content Brief]
- [7]. Hoeferlin LA, et al. Challenges in the treatment of triple negative and HER2-overexpressing breast cancer. J Surg Sci. 2013;1:3-7. [Content Brief]
- [8]. Hickinson DM, et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer. Clin Cancer Res. 2010 Feb 15;16(4):1159-69. [Content Brief]
- [9]. Menendez JA, et al. Trastuzumab in combination with heregulin-activated Her-2 (erbB-2) triggers a receptor-enhanced chemosensitivity effect in the absence of Her-2 overexpression. J Clin Oncol. 2006;24(23):3735-3746.
- [10]. Drago JZ, et al. Beyond HER2: Targeting the ErbB receptor family in breast cancer. Cancer Treat Rev. 2022 Sep;109:102436. [Content Brief]
- [11]. Menendez JA, et al. Trastuzumab in combination with heregulin-activated Her-2 (erbB-2) triggers a receptor-enhanced chemosensitivity effect in the absence of Her-2 overexpression. J Clin Oncol. 2006;24(23):3735-3746.
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ErbB2/HER2 Inhibitors
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ErbB2/HER2 Related Products (160)
Related Products (160)
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Recombinant Proteins (40)
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Antibodies (1)
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COVA208
0 ImagesCat. No.: HY-P991234COVA208 is a bispecific FynomAb (a fusion protein of an antibody and a Fyn SH3-derived binding protein) that targets HER2. COVA208 induces the degradation of HER2, reduces the levels of HER2, HER3, and EGFR, thereby effectively blocking the downstream signaling pathways of HER2, including the HER3-PI3K-AKT and MAPK pathways, and simultaneously inducing apoptosis of tumor cells. COVA208 is promising for research of cancers, such as HER2-positive breast cancer, gastric cancer, and colorectal cancer.
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BMS-599626 dihydrochloride
0 ImagesCat. No.: HY-110333CAS No.: 1781932-33-9BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2 overexpressed tumor models.
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Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1)
0 ImagesCat. No.: HY-P990248Purity: 98.53%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.
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EGFR/HER2-IN-5
0 ImagesCat. No.: HY-147994CAS No.: 1879071-97-2EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research.
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Trastuzumab-DM21
0 ImagesCat. No.: HY-185780Synonyms: T-DM21Trastuzumab-DM12 (T-DM21) is an antibody-drug conjugate (ADC). Trastuzumab-DM12 binds to HER2, inhibits HER2 shedding, and mediates antibody-dependent cellular cytotoxicity. Trastuzumab-DM12 is formed by conjugating the antibody Trastuzumab (HY-P9907) with DM-21 (HY-139441). Trastuzumab-DM12 can be used for cancer research.
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HER2-IN-12
0 ImagesCat. No.: HY-151162CAS No.: 2820126-51-8HER2-IN-12 is a HER2 inhibitor (IC50: 121 nM). HER2-IN-12 can be used in the research of cancers, such as breast cancer.
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NODAGA-NHS
0 ImagesCat. No.: HY-156991CAS No.: 1407166-70-4Synonyms: NODA-GA-NHS esterNODAGA-NHS (NODA-GA-NHS ester) is the activated ester form of the NODAGA chelator. NODAGA-NHS conjugates with Trastuzumab (HY-P9907) to form NODAGA-Trastuzumab, a conjugate that can chelate 64Cu for the preparation of radiotracers. NODAGA-NHS covalently binds to the amino group of lactosamine derivatives to form radiotracer precursors. [64Cu]NODAGA-trastuzumab enables PET imaging of tumors expressing HER2. NODAGA-NHS is used in studies of HER2-positive breast cancer and ovarian adenocarcinoma.
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Multi-kinase-IN-4
0 ImagesCat. No.: HY-149407Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer.
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WGYRGFYC
0 ImagesCat. No.: HY-P11590WGYRGFYC (WC8) is a selective HER2-targeting peptide that binds specifically to HER2 by mimicking the antigen-binding site of trastuzumab. The DOTA precursor of WGYRGFYC has a KD of 61.20 nM for HER2. WGYRGFYC enables specific and highly sensitive detection of HER2 expression in HER2-positive breast cancer cells and tumor tissues, and monitors the dynamic downregulation of HER2 expression. WGYRGFYC rapidly distributes to target tissues and is efficiently cleared from non-target tissues via the kidneys, generating an ideal tumor-to-background ratio in imaging; it is a component of the PET radiotracer Ga-DOTA-WC8. WGYRGFYC exhibits no significant cytotoxicity in breast cancer cells, and can be used for non-invasive imaging diagnosis and therapeutic efficacy evaluation of HER2-positive breast cancer.
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HER2-IN-8
0 ImagesCat. No.: HY-144097CAS No.: 2704630-49-7HER2-IN-8 is a HER-2 inhibitor extracted from patent WO2021179274A1 compound 107. HER2-IN-8 can be used for the research of cancer and inflammation.
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Multi-target kinase-IN-7
0 ImagesCat. No.: HY-178157CAS No.: 301820-47-3Multi-target kinase-IN-7 (Compound 1e) is an orally active multi-target kinase inhibitor (IC50 values: CDK2=0.314 μM, EGFR=0.183 μM, HER-2=0.197 μM, VEGFR-2=0.235 μM). Multi-target kinase-IN-7 is promising for research of solid tumors (e.g., lung, breast, prostate cancer).
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Herceptide
0 ImagesCat. No.: HY-P10648CAS No.: 3027722-28-4Synonyms: HER2-targeting peptideHerceptide (HER2-targeting peptide) is a HER2-targeting peptide, and can be further conjugated to the near-infrared fluorescent dye indocyanine green (HY-D0711) (ICG) for developing theranostic agents.
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Pertuzumab-LD3
0 ImagesCat. No.: HY-185460Pertuzumab-LD3 is a humanized antibody-drug conjugate (ADC) targeting HER2. Pertuzumab-LD3 consists of the anti-HER2 humanized IgG1 monoclonal antibody Pertuzumab (HY-P9912), the cleavable linker Gly-Gly-Phe-Gly (HY-P3669), and the PI3K/mTOR-IN-21 (HY-185456) payload. Pertuzumab-LD3 can be used in research on metastatic HER2-positive breast cancer.
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(E/Z)-CP-724714
0 ImagesCat. No.: HY-W008914CAS No.: 537705-08-1(E/Z)-CP-724714 is a racemic compound of (E)-CP-724714 and (Z)-CP-724714 isomers. CP-724714 is a potent and selective orally active ErbB2 (HER2) inhibitor.
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EGFR/HER2-IN-10
0 ImagesCat. No.: HY-157399CAS No.: 2931499-82-8EGFR/HER2-IN-10 (compound 9F) is a potent and selective dual EGFR/HER2 inhibitor with IC50s of 2.3 nM and 234 nM for EGFR and HER2, respectively. EGFR/HER2-IN-10 shows an effective antiproliferative action against prostate carcinoma.
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ErbB-2-binding peptide-2
0 ImagesCat. No.: HY-P12120CAS No.: 499773-67-0Synonyms: KCCYSLErbB-2-binding peptide-2 (KCCYSL) is a peptide targeting ErbB-2/HER2, which specifically binds to the extracellular domain of HER2 and accumulates in HER2-expressing cancer cells. When radiolabeled, ErbB-2-binding peptide-2 serves as a SPECT/CT and PET imaging agent, enabling the visualization of HER2-expressing tumor xenografts. ErbB-2-binding peptide-2 is applicable to research related to ovarian cancer and breast cancer.
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Cyclic(YCDGFYACYMDV)
0 ImagesCat. No.: HY-P10793CAS No.: 535959-77-4Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model.
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NM-02
0 ImagesCat. No.: HY-P991239NM-02 is an antibody targeting HER2 with an EC50 value of 1.2 nM. NM-02 binds to domains I and II of HER2-ECD, blocking HER2-related signaling pathways. NM-02 is promising for research of HER2-positive breast cancer.
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GW837016X
0 ImagesCat. No.: HY-129288CAS No.: 833473-68-0Synonyms: NEU-391GW837016X (NEU-391) is an orally active ErbB-2 kinase covalent inhibitor. GW837016X also is a potent antitrypanosome agent. GW837016X inhibits mitosis and cytokinesis.
