Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0EZAHL
ADC Name
SA-7-49
Synonyms
SA-7-49
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Organization
ShanghaiTech University.
Drug Status
Investigative
Drug-to-Antibody Ratio
4.3
Structure
Antibody Name
Sacituzumab
  Antibody Info 
Antigen Name
Tumor-associated calcium signal transducer 2 (TACSTD2)
  Antigen Info 
Payload Name
Exatecan
  Payload Info 
Therapeutic Target
DNA topoisomerase 1 (TOP1)
  Target Info 
Linker Name
BVP-PEG-VC-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 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
28.28
nM
CVCL_1639
Pancreatic ductal adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
31.59
nM
CVCL_1638
Pancreatic ductal adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 28.28 nM High TROP2 expression (TROP2 +++)
Method Description
Panc 08.13, Panc 10.05, A375 and HCT116 cells were seeded in 96-well plate at a density of 5000 cells per well. After overnight adherence at 37 °C in a humidified incubator with 5 % CO2, drugs were added to the cells in a specific concentration gradient. After incubated at 37 °C, 5 % CO2 for 72h, cell viability was detected using the Cell Counting Kit-8 kit (Shandong Sparkjade Biotechnology Co., Ltd.), and the absorbance optical density (OD) values at 450 nm were read by a microplate reader (SpectraMax i3, MD, USA). The cell viability rate was calculated according to the following equation: viability % = (ODadministration - ODblank)/ (ODcontrol - ODblank) × 100 %. Olaparib and Adavosertib were purchased from MedChemExpress. KU-60019, Rabusertib, ML323, Berzosertib, RI-1 and AZD7648 were purchased from Selleck.

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In Vitro Model Pancreatic ductal adenocarcinoma Panc 10.05 cells CVCL_1639
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 31.59 nM High TROP2 expression (TROP2 +++)
Method Description
Panc 08.13, Panc 10.05, A375 and HCT116 cells were seeded in 96-well plate at a density of 5000 cells per well. After overnight adherence at 37 °C in a humidified incubator with 5 % CO2, drugs were added to the cells in a specific concentration gradient. After incubated at 37 °C, 5 % CO2 for 72h, cell viability was detected using the Cell Counting Kit-8 kit (Shandong Sparkjade Biotechnology Co., Ltd.), and the absorbance optical density (OD) values at 450 nm were read by a microplate reader (SpectraMax i3, MD, USA). The cell viability rate was calculated according to the following equation: viability % = (ODadministration - ODblank)/ (ODcontrol - ODblank) × 100 %. Olaparib and Adavosertib were purchased from MedChemExpress. KU-60019, Rabusertib, ML323, Berzosertib, RI-1 and AZD7648 were purchased from Selleck.

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In Vitro Model Pancreatic ductal adenocarcinoma Panc 08.13 cells CVCL_1638
References
Ref 1 Exploiting synthetic lethality in PDAC with antibody drug conjugates and ATR inhibition