General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ROAIL
ADC Name
AU2017363246B2 Conjugate28
Synonyms
Conjugate28
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Organization
MERSANA THERAPEUTICS, INC.
Drug Status
Investigative
Drug-to-Antibody Ratio
2.8
Structure
Antibody Name
Trastuzumab
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 Antigen Info 
Payload Name
AU2017363246B2+Conjugate28+Payload
 Payload Info 
Linker Name
Undisclosed
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
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) 
< 300
nmol/L
CVCL_0179
Invasive breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
< 300
nmol/L
CVCL_0033
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
< 300
nmol/L
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
< 300
nmol/L
CVCL_2077
Breast ductal carcinoma
Half Maximal inhibitory Concentration (lC50) 
< 300
nmol/L
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) < 300 nmol/L High her2 expression (her2 +++)
Method Description
BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting

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In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 300 nmol/L High her2 expression (her2 +++)
Method Description
SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 300 nmol/L High her2 expression (her2 +++)
Method Description
N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting

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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) < 300 nmol/L Moderate her2 expression (her2++)
Method Description
JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 300 nmol/L Low her2 expression (her2+)
Method Description
MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Peptide-containing linkers for antibody-drug conjugates