General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0QMTOA
ADC Name
Trastuzumab-Example 2
Synonyms
Trastuzumab-Example 2
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Organization
Novartis
Drug Status
Investigative
Drug-to-Antibody Ratio
4
Structure
Antibody Name
Trastuzumab
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 Antigen Info 
Payload Name
CN119343152A 1C1-Example1 Payload
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
CN119343152A 1C1-Example2 Linker
 Linker Info 
Conjugate Type
Cysteine-maleimide conjugation
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.117
nM
CVCL_1603
Gastric tubular adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.117 nM High HER2 expression (HER2 +++)
Method Description
Cultivate the cell line in a tissue culture incubator at 5% CO2 and 37 °C in the optimal growth medium. Separate cells at least 2 days prior to inoculation for proliferation assays to ensure optimal growth density. On the day of vaccination, cell viability and cell density were determined using a cell counter (Vi Cell XR Cell viability analyzer, Beckman Coulter). Inoculate cells with vitality above 85% into a 384 well TC treated plate (Corning catalog number 3765) with a white transparent bottom. Inoculate cells at a density of 1000 cells per well into 45 u L of standard growth medium. Incubate the plate overnight in a tissue culture incubator at 5% CO2 and 37 °C. On the second day, prepare free atorvastatin payload and targeted ADC at a 10 fold ratio in standard growth medium. Add the prepared treatment substance to the cells to obtain a final concentration of 0.005-100nM and a final volume of 50 u L/well. Each drug concentration is tested in quadruplicate. Incubate the plates in a tissue culture incubator at 5% CO2 and 37 °C for 5 days, and then evaluate cell viability by adding 25 u L of CellTiterGlo (Promega, catalog number G7573) (a reagent for cell lysis and measurement of total adenosine triphosphate (ATP) content). Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal, and then read using a luminescence reader (EnVision multi label enzyme-linked immunosorbent assay, PerkinElmer). To evaluate the effectiveness of drug treatment, luminescence counts from wells containing untreated cells (100% viability) were used to normalize the treated samples. Apply a variable slope model to fit the nonlinear regression curve to the data in GraphPad PRISM version 7.02 software. Extrapolating IC50 from the obtained curve

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
References
Ref 1 Antibody-drug conjugates