General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0HCSHN
ADC Name
WO2021147993A1 ADC-7
Synonyms
WO2021147993A1 ADC 7
   Click to Show/Hide
Organization
Jiangsu Hengrui Pharmaceuticals Co., Ltd.
Drug Status
Investigative
Indication
In total 2 Indication(s)
Gastric cancer [ICD11:2B72]
Investigative
Pancreatic cancer [ICD11:2C10]
Investigative
Drug-to-Antibody Ratio
3.72
Structure
Antibody Name
hRS7
 Antibody Info 
Antigen Name
Tumor-associated calcium signal transducer 2 (TACSTD2)
 Antigen Info 
Payload Name
Undisclosed
Linker Name
WO2021147993A1 ADC-7 linker
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
%
COLO 205 cells
Colon adenocarcinoma
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) 
0.18
nM
HCC827 cells
Lung adenocarcinoma
Half Maximal Effective Concentration (EC50) 
0.31
nM
FaDu cells
Hypopharyngeal squamous cell carcinoma
Half Maximal Effective Concentration (EC50) 
50
nM
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Half Maximal Effective Concentration (EC50) 
52.75
nM
COLO 205 cells
Colon adenocarcinoma
Half Maximal Effective Concentration (EC50) 
72.92
nM
DMS 53 cells
Lung small cell carcinoma
Half Maximal Effective Concentration (EC50) 
> 100
nM
CHO-K1 cells
Normal
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 28) Moderate TROP2 expression (TROP2 ++)
Method Description
Conjugates of the exemplary anti-TROP2 antibodies were tested using an established xenograft model of NUGC4 cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model Colo205 CDX model
In Vitro Model Colon adenocarcinoma COLO 205 cells CVCL_0218
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) 0.18 nM High TROP2 expression (TROP2 +++)
Method Description
Conjugate in various concentrations was added to TROP2-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.31 nM High TROP2 expression (TROP2 +++)
Method Description
Conjugate in various concentrations was added to TROP2-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 50.00 nM Positive TROP2 expression (TROP2 +++/++)
Method Description
Conjugate in various concentrations was added to TROP2-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 52.75 nM Moderate TROP2 expression (TROP2 ++)
Method Description
Conjugate in various concentrations was added to TROP2-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Colon adenocarcinoma COLO 205 cells CVCL_0218
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 72.92 nM Moderate TROP2 expression (TROP2 ++)
Method Description
Conjugate in various concentrations was added to TROP2-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Lung small cell carcinoma DMS 53 cells CVCL_1177
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Negative TROP2 expression (TROP2 -)
Method Description
Conjugate in various concentrations was added to TROP2-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Normal CHO-K1 cells CVCL_0214
References
Ref 1 Anti-trop-2 antidody-exatecan analog conjugate and medical use thereof; 2021-07-29.

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