Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0JDEVM
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| ADC Name |
Cet-DM1
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| Synonyms |
Cetuximab-DM1
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| Drug Status |
Investigative
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| Indication |
In total 1 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
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| Drug-to-Antibody Ratio |
3.5
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| Structure |
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| Antibody Name |
Cetuximab
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Antibody Info | ||||
| Antigen Name |
Epidermal growth factor receptor (EGFR)
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Antigen Info | ||||
| Payload Name |
Mertansine DM1
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
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Linker Info | ||||
| Conjugate Type |
Random conjugation through nucleophilic lysines.
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| Combination Type |
Emtansine
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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 Inhibitory Concentration (IC50) | 0.85 nM | High EGFR expression (EGFR+++/++) | ||
| Method Description |
HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
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| In Vivo Model | HCC1954/TDR CDX model (CDX: C#10) | ||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 T-DM1R (T-DM1 resistance) cells | CVCL_1259 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.85 nM | High EGFR expression (EGFR+++/++) | ||
| Method Description |
HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
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| In Vivo Model | HCC1954/TDR CDX model (CDX: C#19) | ||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 T-DM1R (T-DM1 resistance) cells | CVCL_1259 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.41 nM | High EGFR expression (EGFR+++/++) | ||
| Method Description |
HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 3.52 nM | High EGFR expression (EGFR+++/++) | ||
| Method Description |
HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
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| In Vivo Model | HCC1954/TDR CDX model (CDX: C#20) | ||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 T-DM1R (T-DM1 resistance) cells | CVCL_1259 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 7.68 nM | High EGFR expression (EGFR+++/++) | ||
| Method Description |
HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
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| In Vivo Model | HCC1954/TDR CDX model (CDX: C#29) | ||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 T-DM1R (T-DM1 resistance) cells | CVCL_1259 | ||
References
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