SIBP-03
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).
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
Isotype
Human IgG2 kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
[1]|
HER3 |
In Vitro
SIBP-03 (10-4-104 ng/mL) binds strongly and specifically to recombinant human HER3 protein, while no binding is detected with recombinant human EGFR, HER2 or HER4 proteins[1].
SIBP-03 binds to HER3 on the surface of MC38/HER3 cells with overexpressed HER3, while no detectable binding is observed with HER3-negative MC38 cells[1].
SIBP-03 (0.01-10 μg/mL; 24 h treatment of FaDu/BT-474 cells, with 2 h pre-incubation of cells stimulated by NRG1) effectively inhibits ligand-independent and ligand-dependent HER3 activation, as well as the downstream PI3K/AKT signaling pathway, in FaDu, BT-474, and NRG1-stimulated MCF7 and BT-474 cells[1].
SIBP-03 (0.01-100 μg/mL; 120 h) exerts only weak antiproliferative effects on FaDu, A549, BT-474, SK-BR-3 and NCI-N87 cells, but potently inhibits NRG1-stimulated proliferation of MCF7 cells, with an inhibition rate of 74.8% after treatment at 100 μg/mL[1].
SIBP-03 (10-100 μg/mL; 1 h) does not induce complement-dependent cytotoxicity in FaDu cells or HER3-overexpressing MC38/HER3 cells at concentrations of 10 and 100 μg/mL[1].
SIBP-03 (10-100 μg/mL; 5 h) induces ADCC activity in MC38/HER3 cells overexpressing HER3, but fails to induce such activity in BT-474 cells at concentrations of 10 and 100 μg/mL[1].
SIBP-03 (10-100 μg/mL; 5 h) induces antibody-dependent cellular phagocytosis activity in human breast cancer BT-474 cells and HER3-overexpressing MC38/HER3 cells at concentrations of 10 μg/mL and 100 μg/mL[1].
SIBP-03 (30 μg/mL; 144 h) can synergistically enhance the antiproliferative activity of DS-8201 in SK-BR-3 and MDA-MB-453 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Human head and neck squamous cell carcinoma FaDu cells, human non-small cell lung cancer A549 cells, human breast cancer BT-474 cells, human breast cancer SK-BR-3 cells, human gastric cancer NCI-N87 cells, NRG1-stimulated human breast cancer MCF7 cells
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Concentration:0.01-100 μg/mL
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Incubation Time:120 h
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Result:Exhibited weak anti-proliferative effects, with inhibition rates ranging from 10.0% to 32.9% at 100 μg/mL in FaDu, A549, BT-474, SK-BR-3, and NCI-N87 cells.
Induced strong anti-proliferative effects, with 74.8% inhibition at 100 μg/mL in NRG1-stimulated MCF7 cells.
In Vivo
SIBP-03 (6 mg/kg; i.v.) exhibits significant anti-tumor activity in the A549 xenograft mouse model, with a tumor growth inhibition (TGI) rate of 57.5% at the dose of 6 mg/kg[1].
SIBP-03 (20 mg/kg; i.v.) exhibits significant antitumor activity in the NCI-N87 xenograft mouse model, with a tumor growth inhibition (TGI) rate of 50.8% at the dose of 20 mg/kg[1].
Single treatment with SIBP-03 (0.6 mg/kg; i.v.) achieves a TGI of 96% in FaDu xenograft-bearing mice, while combination treatment with Cetuximab (HY-P9905) induces a TGI of 152% and causes tumor regression in 66.7% of treated mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Gene ID
Accession
Target
ERBB3/HER3
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Product Image
Anwendung
ELISA, FACS, Functional assay
Chemical Information
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SMILES
[SIBP-03]
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Reinheit & Dokumentation
Verweise
[1]. Li WJ, et al. SIBP-03, a novel anti-HER3 antibody, exerts antitumor effects and synergizes with EGFR- and HER2-targeted drugs. Acta Pharmacol Sin. 2024;45(4):857-866. [Content Brief]
[2]. Li WJ, et al. HER3 upregulation reduces DS-8201 sensitivity in HER2-positive tumor cells by ATR/CHK1/FoxO1 signaling cascade. Acta Pharmacol Sin. 2026;47(2):481-492. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SIBP-03 Related Classifications
HY-P991984 Related Classifications
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Keywords
- SIBP-03
- SIBP03
- SIBP 03
- EGFR
- PI3K
- Akt
- MC38/HER3 cells
- human tumor xenograft models
- neuregulin
- PI3K/AKT signaling pathway
- HER2-positive tumor cells
- BT-474 human breast cancer cells
- HER3
- antibody-dependent cell-mediated cytotoxicity
- antibody-dependent cellular phagocytosis
- MAPK signaling pathway
- Inhibitor
- inhibitor
- inhibit