Becotatug
Based on 1 Customer Validation
Becotatug (JMT-101) is a humanized IgG1 monoclonal antibody targeting epidermal growth factor receptor (EGFR), and serves as the antibody component of the antibody-drug conjugate Becotatug vedotin (HY-171265). Becotatug specifically binds to the extracellular domain of EGFR, induces receptor internalization and degradation, blocks the EGFR signaling pathway, and mediates antibody-dependent cellular cytotoxicity. When conjugated to monomethyl auristatin E (MMAE) (HY-15162) via a valine-citrulline cleavable linker, Becotatug enables targeted delivery of cytotoxic drugs to EGFR-positive tumor cells. Studies related to Becotatug cover EGFR exon 20 insertion-mutated non-small cell lung cancer, recurrent or metastatic nasopharyngeal carcinoma, recurrent or metastatic head and neck squamous cell carcinoma, and other conditions.
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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。
- 純度: 99.00%
- CAS 番号: 2648260-93-7
- 分子量:145.52 kDa
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
EGFR アイソフォーム固有の製品をすべて表示
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生物活性
Human IgG1 kappa
Human
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EGFR |
Becotatug (JMT-101) (1-200 μg/mL; 72 h) exhibits only extremely weak antiproliferative activity when used alone in EGFR exon 20 insertion mutation-positive Ba/F3 cells[1].
Combined treatment with Becotatug (10 μg/mL; 24 h) and 100 nmol/L Afatinib (HY-10261) or Osimertinib (HY-15772) for 24 hours induces EGFR downregulation and endocytosis in EGFR insASV-positive Ba/F3 cells[1].
Becotatug (10 μg/mL; 6 h) alone does not block the EGFR signaling pathway in EGFR exon 20 insertion-positive Ba/F3 cells, but when combined with 100 nmol/L afatinib or osimertinib, it potently inhibits EGFR pathway activation and reduces total EGFR levels in these cell lines[1].
When co-cultured with natural killer (NK) cells at an effector-to-target cell ratio of 4:1, Becotatug (0.00001-100 μg/mL; 30 min pre-incubation with target cells, followed by 4 h co-culture with NK cells) induces dose-dependent antibody-dependent cell-mediated cytotoxicity in EGFR exon 20 insertion mutation-positive Ba/F3 cells (insASV, insSVD, insNPH)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cells stably expressing EGFR exon 20 insertions (A767_V769dup/insASV, S768_D770dup/insSVD, N771_H773dup/insNPH)
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Concentration:1-200 μg/mL (Becotatug alone); 10 μg/mL (Becotatug in combination with afatinib/osimertinib)
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Incubation Time:72 h
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Result:Had minimal effect on the viability of all three EGFR exon 20 insertion-positive Ba/F3 cell lines when used alone at concentrations from 1 to 200 μg/mL.
Shifted the dose-response curves of afatinib and osimertinib to the left, demonstrating potent antiproliferative effects when used at 10 μg/mL in combination with the TKIs.
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Cell Line:EGFR exon 20 insertion-positive Ba/F3 cells (insASV, insSVD, insNPH)
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Concentration:10 μg/mL (Becotatug alone); 10 μg/mL (Becotatug in combination with 100 nmol/L afatinib or osimertinib)
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Incubation Time:6 h
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Result:Did not efficiently block EGFR signaling activation in the three cell lines when used alone at 10 μg/mL.
Strongly inhibited EGFR signaling activation, including phosphorylation of EGFR, AKT, and ERK1/2, and reduced total EGFR levels when used at 10 μg/mL in combination with 100 nmol/L afatinib or osimertinib.
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Cell Line:EGFR insASV-positive Ba/F3 cells
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Concentration:10 μg/mL (Becotatug alone); 10 μg/mL (Becotatug in combination with 100 nmol/L afatinib or osimertinib)
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Incubation Time:24 h
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Result:Exhibited marked downregulation of total EGFR levels and a trend of EGFR internalization when used at 10 μg/mL in combination with 100 nmol/L afatinib or osimertinib, compared with cells treated with afatinib or osimertinib alone.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG1 kappa
ELISA, FACS, Functional assay
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Loaded Becotatug on AHC2 biosensor, can bind EGFR Protein, Human (621a.a, Sf9, His, HY-P7316) with an affinity constant of 3.430E-09 M as determined in BLI assay. -
Flow Cytometry analysis of A431 cells labelling EGFR (red) with Becotatug (anti-EGFR) (HY-P99049). Goat Anti-Human IgG (Alexa Fluor 488) (HY-P83776) at a dilution of 1/1000 was used as the secondary antibody. Blue-Human IgG1 kappa (HY-P99001). Black-Unlabelled control, cells without incubation with primary antibody.
化学情報
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CAS 番号 2648260-93-7
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性状 Liquid
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分子量 145.52 kDa
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Color Colorless to light yellow
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SMILES
[Becotatug]
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別名
JMT-101; MRG003 Antibody
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輸送条件
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
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データシート (264 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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Inhibitory Antibodies User Guide (603 KB)
参考文献
[2]. Han F, et al. Becotatug vedotin, MRG003, in previously treated recurrent or metastatic nasopharyngeal carcinoma: A multicenter, single-arm, phase IIa trial. Med (New York, N.Y.). 2026 Apr 10;7(4):101029. [Content Brief]
[3]. Qiu MZ, et al. Evaluation of Safety of Treatment With Anti-Epidermal Growth Factor Receptor Antibody Drug Conjugate MRG003 in Patients With Advanced Solid Tumors: A Phase 1 Nonrandomized Clinical Trial. JAMA oncology. 2022 Jul 01;8(7):1042-1046. [Content Brief]
[4]. Xue L, et al. Becotatug Vedotin in Patients with Recurrent or Metastatic Squamous Cell Carcinoma of the Head and Neck: A Multicenter, Phase IIa Trial. Clinical cancer research : an official journal of the American Association for Cancer Research. 2026 Apr 15;32(8):1445-1453. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Becotatug 関連分類
HY-P990049 関連分類
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- Becotatug
- 2648260-93-7
- JMT-101
- MRG003 Antibody
- JMT101
- JMT 101
- EGFR
- nasopharyngeal carcinoma
- non-small-cell lung cancer
- extracellular domain
- EGFR exon 20 insertion-expressing cells
- monomethyl auristatin E
- squamous cell carcinoma of the head and neck
- xenograft models
- valine-citrulline linker
- antibody-dependent cellular cytotoxicity
- Inhibitor
- inhibitor
- inhibit