Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0KSILR
|
|||||
|---|---|---|---|---|---|---|
| ADC Name |
37828728 ADC 1
|
|||||
| Synonyms |
ADC 1
Click to Show/Hide
|
|||||
| Organization |
Planegg-Martinsried.; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP).; Humboldt Universität zu Berlin.
|
|||||
| Drug Status |
Investigative
|
|||||
| Drug-to-Antibody Ratio |
0.28
|
|||||
| Structure |
|
|||||
| Antibody Name |
Trastuzumab
|
Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
|
Antigen Info | ||||
| Payload Name |
Exatecan
|
Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
|
Target Info | ||||
| Linker Name |
P5 (OEt)-VC-PAB
|
Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
|
|||||
| Combination Type |
P5 (OEt)-VC-PAB-exatecan
|
|||||
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) | 251 ng/mL | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).
Click to Show/Hide
|
||||
| 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) | > 3000 ng/mL | Negative HER2 expression (HER2-) | ||
| Method Description |
To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).
Click to Show/Hide
|
||||
| In Vitro Model | Lung adenocarcinoma | HCC-78 cells | CVCL_2061 | ||
References