Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0YPBUS
ADC Name
B9-MMAE
Synonyms
B9-MMAE
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Organization
Fudan University.; University of Auckland,.; Shanghai Engineering Research Center for Synthetic Immunology.
Drug Status
Investigative
Structure
Antibody Name
B9
  Antibody Info 
Antigen Name
Carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5)
  Antigen Info 
Payload Name
Monomethyl auristatin E
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Mc-Val-Cit-PABC
  Linker Info 
Combination Type
Vedotin
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) 
25.6
nM
CVCL_0186
Pancreatic ductal adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
38.14
nM
CVCL_0434
Gastric adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
101.4
nM
CVCL_1384
Colon 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) 25.6 nM Low CEACAM5 expression (CEACAM5+)
Method Description
Logarithmically growing cell lines MKN-45, BxPC-3, LS174T, and FCHO were seeded in a 96 well cell culture plate at 5000 cells/well for 12 h. After the culture supernatant was discarded, the 200 uL three-fold diluted UdADC was added to cells, with native antibody B9 and free payload vcMMAE used as control. The concentration of each group started from 1 uM and was repeated in triplicate. Cells were cultured for 72 h at 37 °C, then the culture medium was removed and 100 uL CCK8 solution (10 uL CCK8 + 90 uL medium) was added into each well, using CCK8 solution without cells as reference wells. After cells were incubated at 37 °C for 1-3 h, absorbance was measured at 450 nm using a 96-well microplate reader. Cell viability (%) = [ (ODtreated - ODreference well)/ (ODnon-treated - ODreference well)] × 100%.

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In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 38.14 nM High CEACAM5 expression (CEACAM5 +++)
Method Description
Logarithmically growing cell lines MKN-45, BxPC-3, LS174T, and FCHO were seeded in a 96 well cell culture plate at 5000 cells/well for 12 h. After the culture supernatant was discarded, the 200 uL three-fold diluted UdADC was added to cells, with native antibody B9 and free payload vcMMAE used as control. The concentration of each group started from 1 uM and was repeated in triplicate. Cells were cultured for 72 h at 37 °C, then the culture medium was removed and 100 uL CCK8 solution (10 uL CCK8 + 90 uL medium) was added into each well, using CCK8 solution without cells as reference wells. After cells were incubated at 37 °C for 1-3 h, absorbance was measured at 450 nm using a 96-well microplate reader. Cell viability (%) = [ (ODtreated - ODreference well)/ (ODnon-treated - ODreference well)] × 100%.

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In Vitro Model Gastric adenocarcinoma MKN-45 cells CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 101.4 nM High CEACAM5 expression (CEACAM5 +++)
Method Description
Logarithmically growing cell lines MKN-45, BxPC-3, LS174T, and FCHO were seeded in a 96 well cell culture plate at 5000 cells/well for 12 h. After the culture supernatant was discarded, the 200 uL three-fold diluted UdADC was added to cells, with native antibody B9 and free payload vcMMAE used as control. The concentration of each group started from 1 uM and was repeated in triplicate. Cells were cultured for 72 h at 37 °C, then the culture medium was removed and 100 uL CCK8 solution (10 uL CCK8 + 90 uL medium) was added into each well, using CCK8 solution without cells as reference wells. After cells were incubated at 37 °C for 1-3 h, absorbance was measured at 450 nm using a 96-well microplate reader. Cell viability (%) = [ (ODtreated - ODreference well)/ (ODnon-treated - ODreference well)] × 100%.

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In Vitro Model Colon adenocarcinoma LS174T cells CVCL_1384
References
Ref 1 A novel human single-domain antibody-drug conjugate targeting CEACAM5 exhibits potent in vitro and in vivo antitumor activity