Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0HZHNS
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| ADC Name |
HER2-18
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| Synonyms |
HER2-18
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| Organization |
Fudan University.; Shanghai Fudan-Zhangjiang Bio-Pharmaceutical Co.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
7.6
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| Structure |
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| Antibody Name |
Trastuzumab
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Antibody Info | ||||
| 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 |
Mc-Val-Cit-PABC
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Linker Info | ||||
| Conjugate Type |
Site-specific conjugation via re-bridging.
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ADC-specific functional property(2027 Update)
Circulating Stability
| Incubation Time | 7day | Release | <1% | Reference |
[1]
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| Incubation Medium | PBS | ||||
| Description |
After considering CPTS-1 and WL-14 as potential effector molecules for ADCs, we conducted stability analyses on their linker-drug complexes connected by Val-Ala and Val-Cit to preliminarily evaluate their stability in the body circulation. Excitingly, our findings demonstrated that all complexes maintained their stability under PBS 7.4 conditions for a duration of 7 days. The maximum release observed was 1.72% for CPTS-1 and a mere 0.91% for WL-14 (Table 2). These results showed the exceptional stability of these complexes, highlighting their potential for use in ADCs.
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Payload Release Efficiency
| Incubation Time | 4h | Release | 100% | Reference |
[1]
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| Description |
To further validate the viability of releasing peptide linkers with quaternary ammonium structures, we conducted in vitro enzymatic release experiments using cathepsin B on HER2-14, HER2-16 ~ HER2-18.
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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) | 67.94䔱.53 ng/mL | High HER2 expression (HER2+++; >300,000 HER2 molecules/cell) | ||
| Method Description |
Cells were distributed into 96-well white round-bottom plates, with each well receiving 1000 cells in RPMI-1640 medium supplemented with 10% FBS. Following a 24-hour incubation period, diluted compounds were introduced to the wells. After 144 hours, a CellTiter-Glo luminescent cell viability assay (Promega, Madison, WI, USA) was performed to assess cell viability. The luminescent readings were normalized as percentages relative to untreated cells, and the IC50 values for each compound were determined.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
References