General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0IJMYA
ADC Name
MSLN-Suc/SPAAC-PEG4-Eribulin
Synonyms
MSLN Suc/SPAAC PEG4 Eribulin
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
2.8
Antibody Name
Amatuximab
 Antibody Info 
Antigen Name
Mesothelin (MSLN)
 Antigen Info 
Payload Name
Eribulin
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Succinamide-SPAAC-PEG4
 Linker Info 
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 (IC50) 
39
nM
NCI-H2110 cells
Lung non-small cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
61
nM
IGROV-1 cells
Ovarian endometrioid adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 100
nM
A431 cells
Skin squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 100
nM
SJSA-1 cells
Osteosarcoma
Half Maximal Inhibitory Concentration (IC50) 
> 100
nM
SJSA-1 cells
Osteosarcoma
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 (IC50) 39.00 nM Moderate MSLN expression(MSLN++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Lung non-small cell carcinoma NCI-H2110 cells CVCL_1530
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 61.00 nM Negative MSLN expression(MSLN-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Ovarian endometrioid adenocarcinoma IGROV-1 cells CVCL_1304
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative MSLN expression(MSLN-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative MSLN expression(MSLN-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma SJSA-1 cells CVCL_1697
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative MSLN expression(MSLN-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma SJSA-1 cells CVCL_1697
References
Ref 1 MORAb-202, an Antibody-Drug Conjugate Utilizing Humanized Anti-human FR Farletuzumab and the Microtubule-targeting Agent Eribulin, has Potent Antitumor Activity. Mol Cancer Ther. 2018 Dec;17(12):2665-2675. doi: 10.1158/1535-7163.MCT-17-1215. Epub 2018 Sep 27.

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