General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0QUVEH
ADC Name
US20230256114A1 ADC (DAR4) 1
Synonyms
US20230256114A1 ADC (DAR4) 1
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Organization
BIONECURE THERAPEUTICS, INC.
Drug Status
Investigative
Drug-to-Antibody Ratio
4
Antibody Name
Anti-Trop
 Antibody Info 
Antigen Name
Tumor-associated calcium signal transducer 2 (TACSTD2)
 Antigen Info 
Payload Name
Mertansine DM1
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Succinimidyl-4- (N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
 Linker Info 
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 12 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.49
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.51
nM
CVCL_0186
Pancreatic ductal adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.54
nM
CVCL_0419
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.68
nM
CVCL_0218
Colon adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
1.01
nM
CVCL_0186
Pancreatic ductal adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
2.88
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
4.88
nM
CVCL_0419
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
56.42
nM
CVCL_0218
Colon adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
> 100
nM
CVCL_0023
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
> 100
nM
CVCL_0062
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
> 100
nM
CVCL_0023
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
> 100
nM
CVCL_0062
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 12 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.49 nM Positive TROP2 expression (TROP2+++/++)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.51 nM High TROP2 expression (TROP2 +++)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.54 nM Moderate TROP2 expression (TROP2++)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.68 nM Low TROP2 expression (TROP2+)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Colon adenocarcinoma Colo205 cells CVCL_0218
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 1.01 nM High TROP2 expression (TROP2 +++)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 2.88 nM Positive TROP2 expression (TROP2+++/++)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 4.88 nM Moderate TROP2 expression (TROP2++)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 56.42 nM Low TROP2 expression (TROP2+)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Colon adenocarcinoma Colo205 cells CVCL_0218
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Negative TROP2 expression (TROP2-)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Lung adenocarcinoma A549 cells CVCL_0023
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Negative TROP2 expression (TROP2-)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Negative TROP2 expression (TROP2-)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Lung adenocarcinoma A549 cells CVCL_0023
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Negative TROP2 expression (TROP2-)
Method Description
Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
References
Ref 1 Novel maytansinoids as ADC payloads and their use for the treatment of cancer