General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0VJZAF
ADC Name
C4-MMAE
Synonyms
C4-MMAE
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Organization
Anhui University of Chinese Medicine.; Biocytogen Pharmaceuticals (Beijing) Co., Ltd.; Yangtze Delta Drug Advanced Research Institute.
Drug Status
Investigative
Drug-to-Antibody Ratio
4
Structure
Antibody Name
C4
 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
Site-specific conjugation via re-bridging.
Combination Type
Vedotin
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 11 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.54
uM
CVCL_0186
Pancreatic ductal adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.54
uM
CVCL_0419
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.85
uM
CVCL_0062
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
3.8
uM
CVCL_0152
Pancreatic ductal adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
10.79
uM
CVCL_1119
Cystic fibrosis, Pancreatic ductal adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.01
ug/mL
CVCL_0037
Skin squamous cell carcinoma
Half Maximal inhibitory Concentration (lC50) 
0.02
ug/mL
CVCL_1483
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.02
ug/mL
CVCL_1511
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.05
ug/mL
CVCL_1633
Pancreatic adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.12
ug/mL
CVCL_0532
Ovarian serous adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
4.18
ug/mL
CVCL_1566
Lung squamous cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 11 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.54 uM Moderate HER2 expression (HER2++)
Method Description
The in vitro antitumor efficacy of ADC was assessed using the BxPc-3 cell.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.54 uM Low HER2 expression (HER2+)
Method Description
The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.85 uM Low HER2 expression (HER2+)
Method Description
The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 3.8 uM Low HER2 expression (HER2+)
Method Description
The in vitro antitumor efficacy of ADC was assessed using the AsPc1 cell.
In Vitro Model Pancreatic ductal adenocarcinoma AsPc1 cells CVCL_0152
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 10.79 uM Moderate HER2 expression (HER2++)
Method Description
The in vitro antitumor efficacy of ADC was assessed using the CFPAC cell.
In Vitro Model Cystic fibrosis, Pancreatic ductal adenocarcinoma CFPAC cells CVCL_1119
Experiment 6 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.01 ug/mL High EGFR expression (EGFR +++)
Method Description
A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.

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In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 7 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.02 ug/mL High EGFR expression (EGFR +++)
Method Description
A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.

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In Vitro Model Lung adenocarcinoma NCI-H1650 cells CVCL_1483
Experiment 8 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.02 ug/mL High EGFR expression (EGFR +++)
Method Description
A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.

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In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 9 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.05 ug/mL Moderate EGFR expression (EGFR++)
Method Description
A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.

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In Vitro Model Pancreatic adenocarcinoma Panc_02_03 cells CVCL_1633
Experiment 10 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.12 ug/mL Moderate EGFR expression (EGFR++)
Method Description
A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.

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In Vitro Model Ovarian serous adenocarcinoma SKOV-3 cells CVCL_0532
Experiment 11 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 4.18 ug/mL Negative EGFR expression (EGFR-)
Method Description
A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.

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In Vitro Model Lung squamous cell carcinoma NCI-H520 cells CVCL_1566
References
Ref 1 A comparison of the activity, lysosomal stability, and efficacy of legumain-cleavable and cathepsin-cleavable ADC linkers
Ref 2 A novel anti-HER2/EGFR bispecific antibody-drug conjugate demonstrates promising antitumor efficacy and overcomes resistance to HER2- or EGFR-targeted ADCs