General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0XQRVQ
ADC Name
ZA202500114A-ADC-1
Synonyms
ZA202500114A-ADC-1
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Organization
GENEQUANTUM HEALTHCARE (SUZHOU) CO., LTD.
Drug Status
Investigative
Drug-to-Antibody Ratio
1.93
Antibody Name
ZA202500114A-mAb-1
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 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
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 lnhibition value (TGl) 
115.07
%
Undisclosed Undisclosed
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) 
0.04636
nM
CVCL_0179
Invasive breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
0.08706
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal Effective Concentration (EC50) 
0.045
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
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 lnhibition value (TGl) 115.07% Positive her2 expression (her2+++/++)
Method Description
Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 1x106 (NCI-N87) tumor cells, and treatment with 3mg/kg ADC after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 35.
In Vivo Model NCI-N87 xenograft model
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 Negativeher2 expression (her2-)
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) 0.04636 nM Positive her2 expression (her2+++/++)
Method Description
BT-474 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 Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.08706 nM Positive her2 expression (her2+++/++)
Method Description
NCI-N87 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 Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.045 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