General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0JDEVM
ADC Name
Cet-DM1
Synonyms
Cetuximab-DM1
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
3.5
Structure
Antibody Name
Cetuximab
 Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR)
 Antigen Info 
Payload Name
Mertansine DM1
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
 Linker Info 
Conjugate Type
Random conjugation through nucleophilic lysines.
Combination Type
Emtansine
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.85
nM
HCC1954 T-DM1R (T-DM1 resistance) cells
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.85
nM
HCC1954 T-DM1R (T-DM1 resistance) cells
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
1.41
nM
HCC1954 cells
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
3.52
nM
HCC1954 T-DM1R (T-DM1 resistance) cells
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
7.68
nM
HCC1954 T-DM1R (T-DM1 resistance) cells
Breast ductal carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
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.
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.
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.
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.
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.
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
Ref 1 An anti-EGFR antibody-drug conjugate overcomes resistance to HER2-targeted drugs. Cancer Lett. 2023 Feb 1;554:216024.

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