Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0VOPHD
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| ADC Name |
Trz-LC:p67-MMAE
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| Synonyms |
Trz-LC:p67-MMAE
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| Organization |
Technical University of Darmstadt.
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| Drug Status |
Investigative
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| Structure |
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| Antibody Name |
Trz-LC:p67
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Undisclosed
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| Conjugate Type |
Direct preparation of site-specific ADC with unpurified antibodies in culture medium.
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ADC-specific functional property(2027 Update)
Binding Affinity
| Dissocation Constant (Kd) | Binding Target | Description | Reference |
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| 5.2 nM |
SK-BR-3 cells (HER2)
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EC50 values derived from cellular binding assays on SK-BR-3 cells.
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[1]
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General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
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) | 2 nM | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
6000 cells/well were seeded in a U bottom 96 well plate in 90 uL of medium (Table S 2) and incubated over night at 37 °C and 5% CO2. Jurkat cells utilized for this assay were derived from mechanism-of-action (MOA)-based bioassay core kit to measure FcGammaRIIIa (V158) function (Promega GmbH, Walldorf, Germany). The next day, 10 uL of a dilution row of each sample was added and cells were incubated for 3 days at 37°C and 5% CO2. To evaluate viability, cellular viability assay was performed utilizing CellTiter-Blue® (Promega GmbH, Walldorf, Germany) following the instructions if the supplier. Fluorescence measurement was conducted with a CLARIOstar Plus (BMG Labtech, Ortenberg, Germany) plate reader. Experiments with SKBR3, A431 and Ramos were conducted in at least two biological replicates with three technical replicates each. Assays on Jurkat cells were performed in technical triplicates.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 7.2 nM | Low HER2 expression (HER2+) | ||
| Method Description |
6000 cells/well were seeded in a U bottom 96 well plate in 90 uL of medium (Table S 2) and incubated over night at 37 °C and 5% CO2. Jurkat cells utilized for this assay were derived from mechanism-of-action (MOA)-based bioassay core kit to measure FcGammaRIIIa (V158) function (Promega GmbH, Walldorf, Germany). The next day, 10 uL of a dilution row of each sample was added and cells were incubated for 3 days at 37°C and 5% CO2. To evaluate viability, cellular viability assay was performed utilizing CellTiter-Blue® (Promega GmbH, Walldorf, Germany) following the instructions if the supplier. Fluorescence measurement was conducted with a CLARIOstar Plus (BMG Labtech, Ortenberg, Germany) plate reader. Experiments with SKBR3, A431 and Ramos were conducted in at least two biological replicates with three technical replicates each. Assays on Jurkat cells were performed in technical triplicates.
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| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 7.6 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
6000 cells/well were seeded in a U bottom 96 well plate in 90 uL of medium (Table S 2) and incubated over night at 37 °C and 5% CO2. Jurkat cells utilized for this assay were derived from mechanism-of-action (MOA)-based bioassay core kit to measure FcGammaRIIIa (V158) function (Promega GmbH, Walldorf, Germany). The next day, 10 uL of a dilution row of each sample was added and cells were incubated for 3 days at 37°C and 5% CO2. To evaluate viability, cellular viability assay was performed utilizing CellTiter-Blue® (Promega GmbH, Walldorf, Germany) following the instructions if the supplier. Fluorescence measurement was conducted with a CLARIOstar Plus (BMG Labtech, Ortenberg, Germany) plate reader. Experiments with SKBR3, A431 and Ramos were conducted in at least two biological replicates with three technical replicates each. Assays on Jurkat cells were performed in technical triplicates.
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| In Vitro Model | Adenocarcinoma of the rat mammary gland | Jurkat Fc-GammaIIIa++ cells | CVCL_3475 | ||
References
