Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0MVZYO
ADC Name
WO2014068443A1 ADC39
Synonyms
WO2014068443A1 ADC39
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Organization
Pfizer Inc.
Drug Status
Investigative
Indication
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Drug-to-Antibody Ratio
3.2
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
Undisclosed
Linker Name
WO2014068443A1_ADC39 linker
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.25
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.81
nM
CVCL_0179
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
539.32
nM
CVCL_0620
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 652.88
nM
CVCL_0419
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.25 nM High HER2 expression (HER2+++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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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 (IC50) 0.81 nM High HER2 expression (HER2+++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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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 (IC50) 539.32 nM Moderate HER2 expression (HER2 ++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Breast adenocarcinoma MDA-MB-361 cells CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 652.88 nM Negative HER2 expression (HER2-)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
References
Ref 1 Spliceostatin analogs.

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