General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0VWVOU
ADC Name
Cetuximab-vc-MMAE
Synonyms
Cetuximab-vcMMAE
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Hepatocellular carcinoma [ICD11:2C12]
Investigative
Drug-to-Antibody Ratio
3-4
Antibody Name
Cetuximab
 Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR)
 Antigen Info 
Payload Name
Monomethyl auristatin E
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Mc-Val-Cit-PABC
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
Vedotin
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Inhibition rate (50 nM) 
92
%
A431 cells
Skin squamous cell carcinoma
Half Maximal Effective Concentration (EC50) 
0.1
nM
A431 cells
Skin squamous cell carcinoma
Half Maximal Effective Concentration (EC50) 
1
nM
NHEK-iPSCs #1 cells
Normal
80% Effective Dose (ED80) 
0.7
nM
A431 cells
Skin squamous cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Inhibition rate (50 nM) 92.00% High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.10 nM High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.00 nM
Method Description
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Normal NHEK-iPSCs #1 cells CVCL_A4HY
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data 80% Effective Dose (ED80) 0.70 nM High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
References
Ref 1 Balancing Selectivity and Efficacy of Bispecific Epidermal Growth Factor Receptor (EGFR) c-MET Antibodies and Antibody-Drug Conjugates. J Biol Chem. 2016 Nov 25;291(48):25106-25119. doi: 10.1074/jbc.M116.753491. Epub 2016 Sep 30.

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