Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0FYIRM
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| ADC Name |
38501590 Anti-HER2 ARC-FDC (2)
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| Synonyms |
Anti-HER2 ARC-FDC (2)
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| Organization |
University of Southern California; University of California, Irvine
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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 |
Trastuzumab-Fab-cd38
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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 F
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
2'-Cl-araNAD linker
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Linker Info | ||||
| Conjugate Type |
Site-specific bioconjugation via benzylguanine based autocatalytic covalent conjugation.
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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 Effective Concentration (EC50) | 1.39۪.44 nM | High HER2 expression (HER2 +++) | ||
| Method Description |
Human breast cancer cells in passage 4 or 5 or U937 cells in passage 3 were seeded in 96-well culture plates at a density of 15,000 cells/well in 90 uL culture media. Cells were then treated in duplicates with anti-HER2 ARC-FDCs, anti-HER2 Fab, anti-HER2 Fab-CD38 fusions, or MMAF-alkyne that were prepared in 3-fold serial dilution starting from 300 nM. Cells treated with 5 uM paclitaxel (MilliporeSigma, MA) and PBS were included for 0% and 100% viability controls, respectively. Following incubation at 37°C in an incubator with 5% CO2 for 72 h, cells were added with MTT (3- (4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) reagent (Thermo Fisher Scientific, MA), incubated for 3 h, and lysed with 20% SDS in 50% dimethylformamide. Absorbance at 580 nm was then measured with a Synergy H1 plate reader after 1-hour incubation at 37°C with 5% CO2. EC50 was calculated by the three-parameter nonlinear regression fitting in GraphPad Prism Version 9.4.0 (GraphPad software, CA).
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 100 nM | Low HER2 expression (HER2+) | ||
| Method Description |
Human breast cancer cells in passage 4 or 5 or U937 cells in passage 3 were seeded in 96-well culture plates at a density of 15,000 cells/well in 90 uL culture media. Cells were then treated in duplicates with anti-HER2 ARC-FDCs, anti-HER2 Fab, anti-HER2 Fab-CD38 fusions, or MMAF-alkyne that were prepared in 3-fold serial dilution starting from 300 nM. Cells treated with 5 uM paclitaxel (MilliporeSigma, MA) and PBS were included for 0% and 100% viability controls, respectively. Following incubation at 37°C in an incubator with 5% CO2 for 72 h, cells were added with MTT (3- (4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) reagent (Thermo Fisher Scientific, MA), incubated for 3 h, and lysed with 20% SDS in 50% dimethylformamide. Absorbance at 580 nm was then measured with a Synergy H1 plate reader after 1-hour incubation at 37°C with 5% CO2. EC50 was calculated by the three-parameter nonlinear regression fitting in GraphPad Prism Version 9.4.0 (GraphPad software, CA).
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||