Becotatug (powder)
Becotatug (powder) (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 (powder) 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 (powder) enables targeted delivery of cytotoxic drugs to EGFR-positive tumor cells. Becotatug (powder) can be used for research related to non-small cell lung cancer, nasopharyngeal carcinoma, and head and neck squamous cell carcinoma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
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Speicherung:
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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Biologische Aktivität
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Chemical Information
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
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EGFR |
In Vitro
Becotatug (JMT-101) (1-200 μg/mL; 72 h) (powder) 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) (powder) 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) (powder) 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) (powder) 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.
Chemical Information
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SMILES
[Becotatug (powder)]
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Synonyms
JMT-101 (powder); MRG003 Antibody (powder)
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Becotatug (powder) Related Classifications
HY-P990049A Related Classifications
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Keywords
- Becotatug (powder)
- JMT-101 (powder)
- MRG003 Antibody (powder)
- 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