Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0KQOWQ
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| ADC Name |
HER2-11
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| Synonyms |
HER2-11
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| Organization |
East China Normal University.; Innovation Center for AI and Drug Discovery.; ATLATL Innovation Center.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
7.5
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| Structure |
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| Antibody Name |
undisclosed
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| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
WL-14
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Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase I (TOP1)
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Target Info | ||||
| Linker Name |
Undisclosed
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| Conjugate Type |
Site-specific bioconjugation via THIOMAB.
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ADC-specific functional property(2027 Update)
Circulating Stability
| Incubation Time | 7day | Release | 1.02% | Reference |
[1]
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| Incubation Medium | Mouse plasama | ||||
| Description |
A small amount of WL-14 was released in the previous stability assay of the drug-linker complex. To further explore the stability of ADC after coupling with the antibody, a mouse plasma stability test was performed on the corresponding ADC. HER2-11 exhibited notable plasma stability with 1.0 % WL-14 released in mouse plasma over 7 days (Table 3), allowing for further biological evaluation.
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| Incubation Time | 5day | Release | 0.84% | Reference |
[1]
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| Incubation Medium | Mouse plasama | ||||
| Description |
A small amount of WL-14 was released in the previous stability assay of the drug-linker complex. To further explore the stability of ADC after coupling with the antibody, a mouse plasma stability test was performed on the corresponding ADC. HER2-11 exhibited notable plasma stability with 1.0 % WL-14 released in mouse plasma over 7 days (Table 3), allowing for further biological evaluation.
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| Incubation Time | 3day | Release | 0.59% | Reference |
[1]
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| Incubation Medium | Mouse plasama | ||||
| Description |
A small amount of WL-14 was released in the previous stability assay of the drug-linker complex. To further explore the stability of ADC after coupling with the antibody, a mouse plasma stability test was performed on the corresponding ADC. HER2-11 exhibited notable plasma stability with 1.0 % WL-14 released in mouse plasma over 7 days (Table 3), allowing for further biological evaluation.
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Payload Release Efficiency
| Incubation Time | 5h | Release | 100% | Reference |
[1]
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| Description |
In order to further investigate the drug release potential of quaternary ammonium salt-based linkers incorporating MAC self-eliminating spacer groups, an in vitro enzymatic release experiment with cathepsin B was performed on the drug-linker complex 11. Fig. 4 illustrates that compound 11, which features the novel quaternary ammonium structure, can completely release WL-14 in the presence of cathepsin B within 5 h. This evidence substantiates the viability of the drug release mechanism associated with the novel quaternary ammonium structure.
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General Information of The Activity Data Related to This ADC
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 77.81 nM | High HER2 expression (HER2+++; >300,000 HER2 molecules/cell) | ||
| Method Description |
Cells were plated into 96-well white round-bottom plates in RPMI-1640 medium supplemented with 10 % FBS. 24 h later, compounds were added to the 96-well plates. Following a 120h incubation period, cell viability was evaluated by a CellTiter-Glo luminescent cell viability assay (Promega, Madison, WI, USA) and the EC50 values of each compound were determined.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
References