General Information of This Antibody
Antibody ID
ANI0KKTWC
Antibody Name
hRS7
Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Humanized IgG1
Antigen Name
Tumor-associated calcium signal transducer 2 (TACSTD2)
 Antigen Info 
Click to Show/Hide the Sequence Information of This Antibody
Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
WO2021147993A1 ADC-6 [Investigative]
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) ≈ 0% 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
WO2021147993A1 ADC-8 [Investigative]
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) ≈ 76% 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
WO2021147993A1 ADC-7 [Investigative]
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% 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 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
hRS7 ATAC 1 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.04 nM
Moderate TROP2 expression (TROP2++)
Method Description
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.

   Click to Show/Hide
In Vitro Model Pancreatic ductal adenocarcinoma Capan-2 cells CVCL_0026
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.05 nM
High TROP2 expression (TROP2 +++)
Method Description
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.

   Click to Show/Hide
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.06 nM
High TROP2 expression (TROP2 +++)
Method Description
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.

   Click to Show/Hide
In Vitro Model Pancreatic ductal adenocarcinoma Capan-1 cells CVCL_0237
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Moderate TROP2 expression (TROP2++)
Method Description
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.

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In Vitro Model Pancreatic ductal adenocarcinoma Capan-2 cells CVCL_0026
hRS7 ATAC 2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.1 nM
Moderate TROP2 expression (TROP2++)
Method Description
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.

   Click to Show/Hide
In Vitro Model Pancreatic ductal adenocarcinoma Capan-2 cells CVCL_0026
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.2 nM
High TROP2 expression (TROP2 +++)
Method Description
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.

   Click to Show/Hide
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.2 nM
High TROP2 expression (TROP2 +++)
Method Description
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.

   Click to Show/Hide
In Vitro Model Pancreatic ductal adenocarcinoma Capan-1 cells CVCL_0237
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Effective Concentration (EC50)
138 nM
Moderate TROP2 expression (TROP2++)
Method Description
Cells were seeded at a density of 2 × 103 cells/well in 90 uL of the respective culture medium. On the following day, cells were exposed to ATACs and incubated at 37°C and 5% CO2 with serial dilutions from 1 × 10-7 mol/L to 1.28 × 10-12 mol/L of the ATACs for 96 hours. Cell proliferation was assessed by the BrdU chemiluminescent ELISA assay (Roche; Sigma-Aldrich/Merck, Cat. # 1669915001), according to the manufacturer's instructions. Luminescence signal intensities were measured directly in a microplate reader (BMG CLARIOstar). Triplicate wells were used for each treatment, and viability was normalized to untreated cells. Error was calculated as the SEM of three independent experiments.

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In Vitro Model Pancreatic ductal adenocarcinoma Capan-2 cells CVCL_0026
References
Ref 1 Anti-trop-2 antidody-exatecan analog conjugate and medical use thereof; 2021-07-29.
Ref 2 Novel Amanitin-Based Antibody-Drug Conjugates Targeting TROP2 for the Treatment of Pancreatic Cancer