Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0SVBPC
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| ADC Name |
Tra-CAST-MMAE
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| Synonyms |
Tra-CAST-MMAE
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| Organization |
Fudan University.; Westlake Laboratory of Life Sciences and Biomedicine.; Westlake University.; Westlake Institute for Advanced Study.; Zhejiang University.; University of California at San Francisco.
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| Drug Status |
Investigative
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| Structure |
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| Antibody Name |
Tra-CAST
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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 |
Styrylboronic acid-Val-Cit-PAB
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Linker Info | ||||
| Conjugate Type |
Site-sepecific conjugation via SPAAC reaction.
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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) | 0.2 nM | High HER2 expression (HER2 +++) | ||
| Method Description |
Cells were seeded in a 96-well white opaque plate at a density of 5 × 103/well (CHO, ATCC, CCL-61) or 1 × 104/well (MCF7 (ATCC, HTB-22), SK-BR-3 (ATCC, HTB-30), SK-OV-3 (ATCC, HTB-77) or JIMT-1 (Beyotime, C6453)). Cells were allowed to attach for 24 h at 37 °C and 5% CO2 in humidified atmosphere. Cells were then treated with serial dilutions of Tra-CAST, Tra-CAST-MMAE and SBA-MMAE or Tra-CASTi, Tra-CASTi-MMAE and DBCO-MMAE for 96 h (BT474, MCF7, SK-BR-3). Cell viability was determined using CellTiter Glo reagents (G7571) and was normalized to the control cells. Data was analyzed by Graphpad software, and the half-maximal effective concentration (EC50) value was calculated by fitting with the log (inhibitor) vs. response module.
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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) | 1.2 nM | High HER2 expression (HER2 +++) | ||
| Method Description |
Cells were seeded in a 96-well white opaque plate at a density of 5 × 103/well (CHO, ATCC, CCL-61) or 1 × 104/well (MCF7 (ATCC, HTB-22), SK-BR-3 (ATCC, HTB-30), SK-OV-3 (ATCC, HTB-77) or JIMT-1 (Beyotime, C6453)). Cells were allowed to attach for 24 h at 37 °C and 5% CO2 in humidified atmosphere. Cells were then treated with serial dilutions of Tra-CAST, Tra-CAST-MMAE and SBA-MMAE or Tra-CASTi, Tra-CASTi-MMAE and DBCO-MMAE for 96 h (BT474, MCF7, SK-BR-3). Cell viability was determined using CellTiter Glo reagents (G7571) and was normalized to the control cells. Data was analyzed by Graphpad software, and the half-maximal effective concentration (EC50) value was calculated by fitting with the log (inhibitor) vs. response module.
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| In Vitro Model | Ovarian serous adenocarcinoma | SKOV-3 cells | CVCL_0532 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 1.7 nM | Positive HER2 expression ( HER2+++/++) | ||
| Method Description |
Cells were seeded in a 96-well white opaque plate at a density of 5 × 103/well (CHO, ATCC, CCL-61) or 1 × 104/well (MCF7 (ATCC, HTB-22), SK-BR-3 (ATCC, HTB-30), SK-OV-3 (ATCC, HTB-77) or JIMT-1 (Beyotime, C6453)). Cells were allowed to attach for 24 h at 37 °C and 5% CO2 in humidified atmosphere. Cells were then treated with serial dilutions of Tra-CAST, Tra-CAST-MMAE and SBA-MMAE or Tra-CASTi, Tra-CASTi-MMAE and DBCO-MMAE for 96 h (BT474, MCF7, SK-BR-3). Cell viability was determined using CellTiter Glo reagents (G7571) and was normalized to the control cells. Data was analyzed by Graphpad software, and the half-maximal effective concentration (EC50) value was calculated by fitting with the log (inhibitor) vs. response module.
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
References