General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0PIAYM
ADC Name
Anti-EGFR-Val-Gln-IGN
Synonyms
Anti EGFR Val Gln IGN
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Drug Status
Investigative
Indication
In total 3 Indication(s)
Lung cancer [ICD11:2C25]
Investigative
Pancreatic ductal adenocarcinoma [ICD11:2C10]
Investigative
Squamous cell cancer [ICD11:2D60-2D61]
Investigative
Drug-to-Antibody Ratio
1.6
Antibody Name
Anti-EGFR mAb
 Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR)
 Antigen Info 
Payload Name
Indolinobenzodiazepine dimer
 Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
 Target Info 
Linker Name
Val-Gln dipeptide linker
 Linker Info 
Conjugate Type
Random conjugation conjugation through nucleophilic lysines.
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Effective Concentration (EC50) 
4.7
pM
SAS cells
Tongue squamous cell carcinoma
Half Maximal Effective Concentration (EC50) 
12
pM
NCI-H292 cells
Lung mucoepidermoid carcinoma
Half Maximal Effective Concentration (EC50) 
13
pM
PC-9 cells
Lung adenocarcinoma
Half Maximal Effective Concentration (EC50) 
14
pM
HSC-2 cells
Oral cavity squamous cell carcinoma
Half Maximal Effective Concentration (EC50) 
39
pM
BxPC-3 cells
Pancreatic ductal adenocarcinoma
Half Maximal Effective Concentration (EC50) 
99
pM
NCI-H1975 cells
Lung adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 4.70 pM Positive EGFR expression (EGFR+++/++)
Method Description
Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model Tongue squamous cell carcinoma SAS cells CVCL_1675
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 12.00 pM Positive EGFR expression (EGFR+++/++)
Method Description
Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 13.00 pM Positive EGFR expression (EGFR+++/++)
Method Description
Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model Lung adenocarcinoma PC-9 cells CVCL_B260
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 14.00 pM Positive EGFR expression (EGFR+++/++)
Method Description
Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model Oral cavity squamous cell carcinoma HSC-2 cells CVCL_1287
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 39.00 pM Positive EGFR expression (EGFR+++/++)
Method Description
Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 99.00 pM Positive EGFR expression (EGFR+++/++)
Method Description
Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
References
Ref 1 Optimizing Lysosomal Activation of Antibody-Drug Conjugates (ADCs) by Incorporation of Novel Cleavable Dipeptide Linkers. Mol Pharm. 2019 Dec 2;16(12):4817-4825. doi: 10.1021/acs.molpharmaceut.9b00696. Epub 2019 Oct 29.

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