Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0HCBIV
ADC Name
aHer2- (AL7-LP9)3.81
Synonyms
33
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Organization
REGENERON PHARMACEUTICALS, INC.
Drug Status
Investigative
Drug-to-Antibody Ratio
3.81
Antibody Name
undisclosed
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
Undisclosed
Therapeutic Target
Stimulator of interferon genes protein (STING1)
  Target Info 
Linker Name
aHer2- (AL7-LP2)<sub>3.83</sub> Linker
  Linker Info 
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 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.14
nM
CVCL_0033
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.661
nM
CVCL_0609
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.82
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
> 400
nM
CVCL_1511
Lung 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 (lC50) 0.14 nM Positive HER2 expression (HER2+++/++)
Method Description
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well SK-BR-3 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.661 nM Positive HER2 expression (HER2+++/++)
Method Description
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well Calu-3 in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.

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In Vitro Model Lung adenocarcinoma Calu-3 cells CVCL_0609
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.82 nM Positive HER2 expression (HER2+++/++)
Method Description
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 1000/well NCI-N87 cells in 80 uL media (target positive cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.

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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) > 400 nM Negative HER2 expression (HER2-)
Method Description
Cells were seeded in their growth media into 96 well plates (Thermo #136101) one day prior to adding ADCs: 800/well NCI-H1975 cells in 80ul media (target negative cells). 20ul assay media diluted ADC/ isotype conjugates (1:4 10 pts starting from 100uM) as well as free drug were transferred to above cells. The plates were incubated at 37°C, 5% CO2 for 6 days.

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In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
References
Ref 1 Prodrugs of topoisomerase I inhibitor for ADC conjugations and methods of use thereof