General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0MGRBJ
ADC Name
HER2-ADC-007
Synonyms
HER2-ADC-007
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Organization
Suzhou Medilink Therapeutics Ltd.
Drug Status
Investigative
Drug-to-Antibody Ratio
1.93;5.85
Structure
Antibody Name
Trastuzumab
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 Antigen Info 
Payload Name
DL012-payload
 Payload Info 
Payload Name
DL003-payload
 Payload Info 
Linker Name
DL012-Linker
 Linker Info 
Linker Name
DL003-Linker
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
DL012;DL003
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth lnhibition value (TGl) 
90.18
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
90.99
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
95.8
%
Undisclosed Undisclosed
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.02
nM
CVCL_0031
Invasive breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
0.02
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.04
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.04
nM
CVCL_0033
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.65
nM
CVCL_1559
Minimally invasive lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
1.85
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
54.6
nM
CVCL_1603
Gastric tubular adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
90.18%
Method Description
Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 5x106 (NCI-H358) tumor cells, and treatment with 1mg/kg (QW&#423) ADC after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 29.
In Vivo Model NCI-H358 xenograft model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
90.99%
Method Description
Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 5x106 (NCI-H358) tumor cells, and treatment with 3mg/kg (QW&#423) ADC after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 29.
In Vivo Model NCI-H358 xenograft model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
95.80%
Method Description
Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 5x106 (NCI-H358) tumor cells, and treatment with 10mg/kg (QW&#423) ADC after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 29.
In Vivo Model NCI-H358 xenograft model
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.02 nM Low her2 expression (her2+)
Method Description
MCF7, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.02 nM Positive her2 expression (her2+++/++)
Method Description
NCIN87 HABCG2, 3000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 200 nM with a 5-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 6 days exposure, 75ul Cell titer glo to test IC50.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.04 nM Positive her2 expression (her2+++/++)
Method Description
NCI N87 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 1000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.

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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 inhibitory Concentration (lC50) 0.04 nM High her2 expression (her2 +++)
Method Description
SKBR3, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.65 nM Low her2 expression (her2+)
Method Description
H358, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.

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In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 1.85 nM Positive her2 expression (her2+++/++)
Method Description
NCI N87, 2000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 300 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 6 days exposure, 75ul Cell titer glo to test IC50.

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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) 54.6 nM Positive her2 expression (her2+++/++)
Method Description
NCIN87 HABCB1, 3000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 5-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 6 days exposure, 75ul Cell titer glo to test IC50.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
References
Ref 1 Multi-payload antibody-drug conjugates and their preparation methods and uses