Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0LBFBM
ADC Name
HER2-ADC-009
Synonyms
HER2-ADC-009
   Click to Show/Hide
Organization
Suzhou Medilink Therapeutics Ltd.
Drug Status
Investigative
Drug-to-Antibody Ratio
2.54;5.41
Structure
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
DL012-payload
  Payload Info 
Payload Name
DL003-payload
  Payload Info 
Linker Name
DL012-Linker
  Linker Info 
Linker Name
DL003-Linker
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
DL012;DL003
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.02
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.02
nM
CVCL_0033
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.32
nM
CVCL_1559
Minimally invasive lung adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.02 nM Positive her2 expression (her2+++/++)
Method Description
NCI N87 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 1000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.

   Click to Show/Hide
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 (lC50) 0.02 nM High her2 expression (her2 +++)
Method Description
SKBR3, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.

   Click to Show/Hide
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) 0.32 nM Low her2 expression (her2+)
Method Description
H358, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.

   Click to Show/Hide
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
References
Ref 1 Multi-payload antibody-drug conjugates and their preparation methods and uses