Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0HKNWF
ADC Name
HD12-SG3249
Synonyms
HD12 SG3249
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 1 Indication(s)
Lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
2
Antibody Name
Anti-MET mAb hD12
  Antibody Info 
Antigen Name
Hepatocyte growth factor receptor (MET)
  Antigen Info 
Payload Name
PBD dimer SG3249
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
Mal-PEG8-Val-Ala-PABC
  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
Maximum inhibition efficiency (MIE) 
76.8
pM
NCI-H1373 cells
Lung adenocarcinoma
Maximum inhibition efficiency (MIE) 
78.7
pM
NCI-H1975 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
21.8
pM
NCI-H1373 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.15
nM
NCI-H1975 cells
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 Maximum inhibition efficiency (MIE) 76.80 pM Moderate MET expression (MET++; IHC H-score=180)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung adenocarcinoma NCI-H1373 cells CVCL_1465
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 78.70 pM Moderate MET expression (MET++; IHC H-score=130)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 21.80 pM Moderate MET expression (MET++; IHC H-score=180)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung adenocarcinoma NCI-H1373 cells CVCL_1465
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.15 nM Moderate MET expression (MET++; IHC H-score=130)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
References
Ref 1 TR1801-ADC: a highly potent cMet antibody-drug conjugate with high activity in patient-derived xenograft models of solid tumors. Mol Oncol. 2020 Jan;14(1):54-68. doi: 10.1002/1878-0261.12600. Epub 2019 Dec 3.

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