Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0MAOTP
ADC Name
ZA202500114A-ADC-4
Synonyms
ZA202500114A-ADC-4
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Organization
GENEQUANTUM HEALTHCARE (SUZHOU) CO., LTD.
Drug Status
Investigative
Drug-to-Antibody Ratio
1.89
Antibody Name
Anti-TROP2 mAb
  Antibody Info 
Antigen Name
Tumor-associated calcium signal transducer 2 (TACSTD2)
  Antigen Info 
Payload Name
Monomethyl auristatin E
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Undisclosed
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 inhibitory Concentration (lC50)  .
nM
CVCL_0027
Hepatoblastoma
Half Maximal inhibitory Concentration (lC50) 
0.09995
nM
CVCL_0186
Pancreatic ductal adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.1297
nM
CVCL_1218
Hypopharyngeal squamous cell carcinoma
Half Maximal Effective Concentration (EC50) 
> 10
nM
CVCL_0034
Embryonal carcinoma
Half Maximal Effective Concentration (EC50) 
> 10
nM
CVCL_0031
Invasive breast 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 inhibitory Concentration (lC50) . nM Negative TROP2 expression (TROP2-)
Method Description
HepG2 at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.

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In Vitro Model Hepatoblastoma HepG2 cells CVCL_0027
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.09995 nM High TROP2 expression (TROP2 +++)
Method Description
BxPC-3 at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.

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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) 0.1297 nM High TROP2 expression (TROP2 +++)
Method Description
FaDu at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.

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In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

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In Vitro Model Embryonal carcinoma Ntera-2 cells CVCL_0034
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 nM Negative ROR1 expression (ROR1-)
Method Description
MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Oligosaccharide linker, linker-payload comprising the same and glycan chain-remodeled antibody-drug conjugate, preparation methods and uses thereof