Patritumab deruxtecan
Based on 1 publication(s) in Google Scholar
Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) targeting HER3, consisting of the anti-HER3 IgG1 antibody Patritumab (HY-P99275), a cleavable tetrapeptide linker, and the membrane-permeable topoisomerase I (Topoisomerase Ⅰ) inhibitor DXd (HY-13631D). After binding to membrane-localized HER3, Patritumab deruxtecan is internalized into lysosomes, where the linker is cleaved to release DXd. DXd enters the nucleus to induce DNA damage and cell death, and exerts a bystander effect via transmembrane diffusion. Patritumab deruxtecan reduces the viability of HER3-positive cells and induces features of immunogenic cell death including CALR membrane exposure, ATP and HMGB1 release, and can be used in studies related to HER3-positive breast cancer and non-small cell lung cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- Antibody:
- 純度 : 99.08%
- CAS 番号: 2227102-46-5
- 分子量:155.24 kDa
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保管条件:Shipping with dry ice
-80°C, protect from light
MedChemExpress(MCE)の使用を引用している文献 Patritumab deruxtecan
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生物活性
製品説明
IC50 & Target
[1]|
HER3 |
Top1 |
体外実験
Patritumab deruxtecan (0.16 µg/mL; 5 days) induces hallmarks of immunogenic cell death, including calreticulin surface exposure, extracellular ATP release, and HMGB1 release, in HER3-overexpressing U2OS cells, but not in parental HER3-negative U2OS cells[3].
Patritumab deruxtecan (0.16 µg/mL; 5 days) induces bystander antitumor effects, reducing viability of HER3-negative U2OS cells when cocultured with HER3-overexpressing U2OS cells[3].
Patritumab deruxtecan (0.16 µg/mL; 5 days) releases its cytotoxic payload DXd into cell culture supernatants when applied to HER3-overexpressing U2OS cells, either alone or in coculture with HER3-negative U2OS cells[3].
Patritumab deruxtecan (0.1-100 nM; 1 h) binds specifically and with comparable affinity to MDA-MB-231 cells expressing HER3 wild type or clinically reported HER3G12C mutations, regardless of HER2 overexpression, with no binding to HER3-negative MDA-MB-231 cells[4].
Patritumab deruxtecan (10 nM; 6 days) significantly inhibits the growth of MDA-MB-231 cells expressing HER3 wild type or most clinically reported HER3 mutations, with activity observed regardless of HER2 overexpression, and no activity against HER3-negative MDA-MB-231 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human osteosarcoma U2OS cells (HER3-negative, differentially tagged), HER3-overexpressing U2OS cells
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Concentration:0.16 µg/mL
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Incubation Time:5 days
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Result:Significantly reduced the viability of both HER3-overexpressing U2OS cells and HER3-negative bystander U2OS cells in the coculture.
Did not affect viability of HER3-negative U2OS cells in monoculture.
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Cell Line:MDA-MB-231 human triple-negative breast cancer cells transduced with HER3 wild type (HER3WT), 11 HER3 mutations, or HER3 empty vector (HER3EV), in the presence or absence of HER2 overexpression
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Concentration:10 nM
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Incubation Time:6 days
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Result:Showed significant growth-inhibitory activity against HER3WT cells.
Exhibited growth-inhibitory activity against most HER3-mutant cells.
Showed no inhibitory activity against HER3EV cells.
Had minimal impact of HER2 overexpression on growth inhibition, though substantial inhibition was not observed in cells expressing HER3 mutations V104M, G325R, and S846I without HER2 overexpression.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Product Details
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Antibody
化学情報
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CAS 番号 2227102-46-5
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性状 Liquid
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分子量 155.24 kDa
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Color Colorless to light yellow
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SMILES
[Patritumab deruxtecan]
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別名
HER3-DXd; U3-1402
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輸送条件
Shipping with dry ice.
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保管条件
-80°C, protect from light
Publications (1)
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Journal Impact Factor
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Most Recent
純度とドキュメンテーション
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データシート (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Jänne PA, et al. Efficacy and Safety of Patritumab Deruxtecan (HER3-DXd) in EGFR Inhibitor-Resistant, -Mutated Non-Small Cell Lung Cancer. Cancer discovery. 2022 Jan;12(1):74-89. [Content Brief]
[2]. Steuer CE, et al. Patritumab Deruxtecan (HER3-DXd; MK-1022) in Non-Small Cell Lung Cancer After Platinum-Based Chemotherapy and Immunotherapy. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2025 Sep;43(25):2816-2826. [Content Brief]
[3]. Forveille S, et al. Patritumab deruxtecan induces immunogenic cell death. Oncoimmunology. 2025 Dec;14(1):2514050. [Content Brief]
[4]. Koyama K, et al. Patritumab deruxtecan (HER3-DXd), a novel HER3 directed antibody drug conjugate, exhibits in vitro activity against breast cancer cells expressing HER3 mutations with and without HER2 overexpression. PloS one. 2022;17(5):e0267027. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Keywords
- Patritumab deruxtecan
- 2227102-46-5
- HER3-DXd
- U3-1402
- Antibody-Drug Conjugates (ADCs)
- EGFR
- Topoisomerase
- Antibody-Drug Conjugates
- ADC
- Epidermal growth factor receptor
- ErbB-1
- HER1
- HER3
- topoisomerase I inhibitor
- immunogenic cell death
- fibrosarcoma
- melanoma
- osteosarcoma
- DNA damage
- non-small cell lung cancer
- apoptosis
- breast cancer
- Inhibitor
- inhibitor
- inhibit