Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0MMRUZ
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| ADC Name |
WO2017089890A1 ADC34
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| Synonyms |
Trastuzumab_compound 25f (DAR 4)
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| Organization |
LegoChem Biosciences, Inc.
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| Drug Status |
Investigative
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| Indication |
In total 3 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Ovarian cancer [ICD11:2C73]
Investigative
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| Drug-to-Antibody Ratio |
4
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| Antibody Name |
Trastuzumab
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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 |
WO2017089890A1_ADC34 linker
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| Conjugate Type |
Site-specific conjugation through nucleophilic lysines.
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 58.68% (Day 36) | Moderate HER2 expression (HER2++) | ||
| Method Description |
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
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| In Vivo Model | JIMT-1 CDX model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 87.39% (Day 36) | Moderate HER2 expression (HER2++) | ||
| Method Description |
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
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| In Vivo Model | JIMT-1 CDX model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.03 nM | High HER2 expression (HER2 +++) | ||
| Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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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 Inhibitory Concentration (IC50) | 0.09 nM | Moderate HER2 expression (HER2++) | ||
| Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.10 nM | Moderate HER2 expression (HER2++) | ||
| Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 33.30 nM | Negative HER2 expression (HER2-) | ||
| Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
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