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. Studies related to Becotatug powder 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.
For research use only. We do not sell to patients.
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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EGFR |
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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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Becotatug (powder) Related Classifications
HY-P990049A Related Classifications
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- Becotatug (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