Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0XWBTY
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| ADC Name |
hRS7 ATAC 1
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| Synonyms |
hRS7 ATAC 1
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| Organization |
Heidelberg Pharma Research GmbH.; Heidelberg Pharma AG.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
2
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| Structure |
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| Antibody Name |
hRS7
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Antibody Info | ||||
| Antigen Name |
Tumor-associated calcium signal transducer 2 (TACSTD2)
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Antigen Info | ||||
| Payload Name |
Alpha-amanitin
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Payload Info | ||||
| Therapeutic Target |
DNA-directed RNA polymerase II subunit RPB2 (POLR2B); DNA-directed RNA polymerase III subunit RPC7 (POLR3G)
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Target Info | ||||
| Linker Name |
Mal-Val-Ala-PAB
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Linker Info | ||||
| Conjugate Type |
Site-specific conjugation via engineered cysteine residues at position D265 (DC) in the Fc part of the antibody
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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) | 0.04 nM | Moderate TROP2 expression (TROP2++) | ||
| Method Description |
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.
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| In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-2 cells | CVCL_0026 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.05 nM | High TROP2 expression (TROP2 +++) | ||
| Method Description |
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.
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| In Vitro Model | Pancreatic ductal adenocarcinoma | BxPC-3 cells | CVCL_0186 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.06 nM | High TROP2 expression (TROP2 +++) | ||
| Method Description |
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.
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| In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-1 cells | CVCL_0237 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 100 nM | Moderate TROP2 expression (TROP2++) | ||
| Method Description |
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.
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| In Vitro Model | Pancreatic ductal adenocarcinoma | Capan-2 cells | CVCL_0026 | ||
References