Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0PAKUQ
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| ADC Name |
Tras-16b
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| Synonyms |
Tras-16b
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| Organization |
East China Normal University.; Shanghai Pharmaceuticals Holding Company Limited.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
7.3
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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 |
14b 39321689
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Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase I (TOP1)
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Target Info | ||||
| Linker Name |
Mc-Gly-Gly-Phe-Gly
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Linker Info | ||||
| Conjugate Type |
Site-specific bioconjugation at Trastuzumab-Lys248-thiol
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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 | Mouse plasama | ||||
| Description |
The stability of the corresponding ADC compounds Tras-16a and Tras-16b in mouse plasma was also assessed. As shown in Table 3, within 7 days, the drug release rates of both Tras-16a and Tras-16b were less than 1 %, confirming that both ADCs exhibit good plasma stability.
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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 inhibitory Concentration (lC50) | 19.33 nM | High HER2 expression (HER2+++; >300,000 HER2 molecules/cell) | ||
| Method Description |
MDA-MB-468, NCI-N87 and SK-BR-3 were seeded per well in a 96-well plate and grew for 24 h. Then cells were exposed to DXd, exatecan, homocamtothecins or Enhertu and further incubated for 72 h. The cell viability and proliferation behavior were assessed by the MTT assay. For each compound, inhibitory concentration values (IC50, EC50) were determined using the GraphPad Prism 6.0 Software for MDA-MB-468, NCI-N87 and SK-BR-3 cells.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
References