Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0KUAHO
ADC Name
Anti-FOLR1-Val-Gln-IGN
Synonyms
Anti FOLR1 Val Gln IGN
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Drug Status
Investigative
Indication
In total 4 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Cervical cancer [ICD11:2C77]
Investigative
Non-small cell lung cancer [ICD11:2C25]
Investigative
Ovarian cancer [ICD11:2C73]
Investigative
Drug-to-Antibody Ratio
1.6
Antibody Name
Anti-FOLR1 mAb
  Antibody Info 
Antigen Name
Folate receptor alpha (FOLR1)
  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 5 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Effective Concentration (EC50) 
3
pM
KB cells
Human papillomavirus-related endocervical adenocarcinoma
Half Maximal Effective Concentration (EC50) 
18
pM
IGROV-1 cells
Ovarian endometrioid adenocarcinoma
Half Maximal Effective Concentration (EC50) 
20
pM
T-47D cells
Invasive breast carcinoma
Half Maximal Effective Concentration (EC50) 
30
pM
OV-90 cells
Ovarian adenocarcinoma
Half Maximal Effective Concentration (EC50) 
50
pM
NCI-H2110 cells
Lung non-small cell 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 Effective Concentration (EC50) 3.00 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 Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 18.00 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 Ovarian endometrioid adenocarcinoma IGROV-1 cells CVCL_1304
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 20.00 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 Invasive breast carcinoma T-47D cells CVCL_0553
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 30.00 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 Ovarian adenocarcinoma OV-90 cells CVCL_3768
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 50.00 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 non-small cell carcinoma NCI-H2110 cells CVCL_1530
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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