Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0RYQBT
ADC Name
Anti-FOLR1-Ala-Ala-IGN
Synonyms
Anti FOLR1 Ala Ala IGN
   Click to Show/Hide
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
Ala-Ala dipeptide
  Linker Info 
Conjugate Type
Random conjugation conjugation through nucleophilic lysines.
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 100
%
NCI-H2110 cells
Lung non-small cell carcinoma
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) 
5
pM
KB cells
Human papillomavirus-related endocervical adenocarcinoma
Half Maximal Effective Concentration (EC50) 
9.3
pM
IGROV-1 cells
Ovarian endometrioid adenocarcinoma
Half Maximal Effective Concentration (EC50) 
30
pM
T-47D cells
Invasive breast carcinoma
Half Maximal Effective Concentration (EC50) 
30
pM
OV-90 cells
Ovarian adenocarcinoma
Half Maximal Effective Concentration (EC50) 
0.2
nM
NCI-H2110 cells
Lung non-small cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) Positive FOLR1 expression (FOLR1+++/++)
Method Description
Animals with established tumors were randomized into six mice per treatment group and dosed with a single i.v. dose of vehicle or IGN ADCs at either 3 ug/kg drug dose.
In Vivo Model NCI-H2110 CDX model
In Vitro Model Lung non-small cell carcinoma NCI-H2110 cells CVCL_1530
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) 5.00 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) 9.30 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) 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 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) 0.20 nM 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.

If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.