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.
For research use only. We do not sell to patients.
- Purity: 99.00%
- CAS No.: 2648260-93-7
- Molecular Weight:145.52 kDa
-
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All EGFR Isoforms
More
Biological Activity
Human IgG1 kappa
Human
|
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.
-
Cell Line:Ba/F3 cells stably expressing EGFR exon 20 insertions (A767_V769dup/insASV, S768_D770dup/insSVD, N771_H773dup/insNPH)
-
Concentration:1-200 μg/mL (Becotatug alone); 10 μg/mL (Becotatug in combination with afatinib/osimertinib)
-
Incubation Time:72 h
-
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.
-
Cell Line:EGFR exon 20 insertion-positive Ba/F3 cells (insASV, insSVD, insNPH)
-
Concentration:10 μg/mL (Becotatug alone); 10 μg/mL (Becotatug in combination with 100 nmol/L afatinib or osimertinib)
-
Incubation Time:6 h
-
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.
-
Cell Line:EGFR insASV-positive Ba/F3 cells
-
Concentration:10 μg/mL (Becotatug alone); 10 μg/mL (Becotatug in combination with 100 nmol/L afatinib or osimertinib)
-
Incubation Time:24 h
-
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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
-
Human IgG1 kappa
ELISA, FACS, Functional assay
-
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.
Chemical Information
-
CAS No. 2648260-93-7
-
Appearance Liquid
-
Molecular Weight 145.52 kDa
-
Color Colorless to light yellow
-
SMILES
[Becotatug]
-
Synonyms
JMT-101; MRG003 Antibody
-
Shipping
Shipping with dry ice.
-
Formulation
Please refer to the lot-specific COA for specific buffer information.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
-
Data Sheet (264 KB)
-
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)
-
Inhibitory Antibodies User Guide (603 KB)
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 Related Classifications
HY-P990049 Related Classifications
Powered by Bioz
- 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