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 Proteins
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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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FS102
0 ImagesCat. No.: HY-P991235Synonyms: BMS-986186FS102 is a selective Fc fragment with antigen binding (Fcab) that targets HER2 with a KD value of 0.8 nM. FS102 induces the degradation of HER2, activates Caspase 3/7 and disrupts the integrity of the cell membrane, triggering apoptosis of tumor cells. FS102 is promising for research of cancers such as breast cancer, gastric cancer, and colorectal cancer.
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TAS-121
0 ImagesCat. No.: HY-164392CAS No.: 1451370-01-6TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models.
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EGFR/HER2/TS-IN-2
0 ImagesCat. No.: HY-146239CAS No.: 2444364-04-7EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylate synthase) inhibitor, with IC50 values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC50 of 1.69 µM.
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EGFR/HER2-IN-4
0 ImagesCat. No.: HY-147992CAS No.: 1879071-89-2EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research.
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EGFR/HER2-IN-3
0 ImagesCat. No.: HY-115952CAS No.: 1031620-09-3EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual inhibitor of EGFR and HER2.
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HER2-IN-18
0 ImagesCat. No.: HY-163419CAS No.: 3031413-03-0HER2-IN-18 is a HER2 inhibitor, with an IC50 less than 200 nM for HER-YVMA and HER-WT. HER2-IN-18 can be used for cancer research.
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HER2-IN-9
0 ImagesCat. No.: HY-143323HER2-IN-9 is an orally active HER2 inhibitor, with an IC50 value of 0.03 μM. HER2-IN-9 inhibits HER-2 positive breast cancer cells proliferation and migration. HER2-IN-9 can be used in the research of breast cancers.
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HER2-IN-20
0 ImagesCat. No.: HY-163657HER2-IN-20 (compound 32) is a potent and selective HER2WT and HER2YVMA inhibitor with IC50 values of 49, 42 nM, respectively. HER2-IN-20 has the potential for the research of non-small cell lung cancer (NSCLC).
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HER2-IN-17
0 ImagesCat. No.: HY-163418CAS No.: 3031412-84-4HER2-IN-17 (Compound 2) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-17 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC).
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HER2-IN-13
0 ImagesCat. No.: HY-153557CAS No.: 2414056-34-9HER2-IN-13 (Compound 33) is an HER2 inhibitor with an IC50 of 8 nM. HER2-IN-13 also inhibits wt-EGFR with an IC50 of 0.40 μM.
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Mefatinib-d6
0 ImagesCat. No.: HY-152852SSynonyms: Mifanertinib-d6Mefatinib-d6 free base (Mifanertinib-d6) is the 6-labeled Mefatinib free base (HY-152852). Mefatinib free base is an orally active EGFR and HER2 kinase inhibitor with IC50 values of 0.4 nM and 11.7 nM, respectively. Mefatinib free base inhibits tumor growth in mouse models of lung cancer xenografts that overexpress EGFR/HER2, carry EGFR mutations, or carry Erlotinib (HY-50896)-resistant EGFR double mutations. Mefatinib free base can be used for the research of advanced EGFR-mutant non-small cell lung cancer.
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EGFR/HER2/DHFR-IN-3
0 ImagesCat. No.: HY-149633EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells.
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EGFR-IN-16
0 ImagesCat. No.: HY-137786CAS No.: 133550-22-8
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EGFR-IN-163
0 ImagesCat. No.: HY-174231EGFR-IN-163 (Compound 13) is a competitive epidermal growth factor receptor (EGFR) inhibitor (IC50=0.079 μM, selective for HER-2 inhibition). EGFR-IN-163 induces tumor cell apoptosis and cell cycle arrest at G₂/M phase. EGFR-IN-163 is promising for research of estrogen receptor-positive (ER+) breast cancer.
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HER2-IN-15
0 ImagesCat. No.: HY-163417CAS No.: 3031412-82-2HER2-IN-15 (Compound 1) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-15 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC).
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HER2-IN-16
0 ImagesCat. No.: HY-163420CAS No.: 3031413-08-5HER2-IN-16 (Compound 14) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-16 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC).
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CP-654577
0 ImagesCat. No.: HY-118900CAS No.: 639087-64-2CP-654577 is a selective ErbB2 inhibitor with an IC50 of 11 nM. CP-654577 downregulates the Notch1 signaling pathway. CP-654577 upregulates p27kip1, reduces the levels of Cyclins D and E, and inhibits G1 phase progression of the cell cycle. CP-654577 induces cell Apoptosis, downregulates activated Akt, and suppresses tumor growth in athymic mice. CP-654577 can be used in breast cancer-related research.
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EGFR/HER2/TS-IN-1
0 ImagesCat. No.: HY-146238CAS No.: 2444363-11-3EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylate synthase) inhibitor with IC50 values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis.
