General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0EBBAG
ADC Name
alpha-cMET FDC-Duo5_P2
Synonyms
alpha-cMET FDC-Duo5_P2
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Organization
Antibody Discovery & Technology, Sorrento Therapeutics, Inc, San Diego, CA, USA.
Drug Status
Investigative
Drug-to-Antibody Ratio
1.8
Structure
Antibody Name
cMET A1-8 IgG Fab
 Antibody Info 
Antigen Name
Hepatocyte growth factor receptor (MET)
 Antigen Info 
Payload Name
Duo5
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Undisclosed
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 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
1.8
nM
CVCL_0078
Gastric 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) 1.8 nM High cMET expression (cMET +++)
Method Description
SNU-5 (1750 cells/well, 12.5 uL), A549 cells (750 cells/well, 12.5 uL), HT-29 (1000 cells/well, 12.5 uL) and SK-BR-3 (1000 cells/well, 12.5 uL) were seeded in a white flat-bottom 384-well plate (3570, Corning) at least 4-8 h before drug treatment for SNU-5 and 16-24 h for all the adherent cells. 2× working stock of the anti-cMET FDC (200 nM) or ADC (20-200 nM) were initially prepared in the cell growth media which were subsequently serially diluted in the corresponding media 3-fold. Following this, 12.5 uL of each of the serially diluted drug conjugates were added into the 384-well plate containing the cells. In a similar manner, replicates of 12.5 uL each of either a 2 uM Staurosporine (S1421, Selleck Chemicals) or media only was added into the wells to serve as the 100% cell killing and 0% cell killing, respectively. For the combination treatment, cells were treated with a 3-fold serial dilution of the anti-cMET IgG starting at 50 nM (final concentration in the well) while holding the FDC concentration constant at the approximate IC50 of 2 nM. After 96 h incubation at 37°C with 5% CO2, 25 uL of room temperature CellTiterGlo2.0 reagent (G9241, Promega) was added to each well using a multichannel pipette followed by a 2-min shaking using an orbital shaker (500 rpm), and then a 10-min incubation at room temperature. Afterwards, the plate was read using plate reader capable of reading luminescence in multi-well plates (Tecan Spark). Data were analyzed using GraphPad Prism software.

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In Vitro Model Gastric adenocarcinoma SNU-5 cells CVCL_0078
References
Ref 1 Discovery of novel cMET-targeting antibody Fab drug conjugates as potential treatment for solid tumors with highly expressed cMET