General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0OKPLP
ADC Name
P015004-vc-PAB-MMAE
Synonyms
#220330
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Organization
AIMED BIO INC.
Drug Status
Investigative
Drug-to-Antibody Ratio
3
Structure
Antibody Name
P015004
 Antibody Info 
Antigen Name
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
 Antigen Info 
Payload Name
Monomethyl auristatin E
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Mc-Val-Cit-PABC
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
Vedotin
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) 
10.62
nM
Undisclosed
lung cancer
Half Maximal inhibitory Concentration (lC50) 
159.5
nM
Undisclosed
lung cancer
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) 10.62 nM High ROR1 expression ( ROR1 +++)
Method Description
In each ultra-low attachment U bottom 384-well transparent plate patient-derived lung cancer cells AMB-LC-0003T were dispensed in triplicate at 500 cells/well in 40 p1l of M10018 (Aimedbio) media. After centrifugation at 250 g for 2 minutes, reaction was carried out at 37°C and 5% Co 2 for 24 hours. Thereafter, each antibody-drug conjugate was serially diluted 3-fold from 500 nM to 0.314 pM and the cells were treated therewith. The plate was reacted again at 37°C and 5% Co2 for 6 days. After a total of 7 days of reaction, spheroids were formed by the cells in the 384-well plate, so images of spheroids in each well were captured using Operetta CLS (PerkinElmer) according to a high-content screening method. To maintain the spheroid form of the cells in each well, washing was not performed before analysis. The captured images were converted into volume through additional analysis, and the spheroid volume values by concentration were standardized based on the spheroid treated with the lowest concentration of drug. Graphs were created with a log (inhibitor) vs. normalized response - Variable slope using GraphPad Prism 9.3.1, and IC5 o values were obtained.

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In Vitro Model lung cancer AMB-LC-0003T cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 159.5 nM Low ROR1 expression (ROR1+)
Method Description
In each ultra-low attachment U bottom 384-well transparent plate patient-derived lung cancer cells AMB-LC-0003T were dispensed in triplicate at 500 cells/well in 40 p1l of M10018 (Aimedbio) media. After centrifugation at 250 g for 2 minutes, reaction was carried out at 37°C and 5% Co 2 for 24 hours. Thereafter, each antibody-drug conjugate was serially diluted 3-fold from 500 nM to 0.314 pM and the cells were treated therewith. The plate was reacted again at 37°C and 5% Co2 for 6 days. After a total of 7 days of reaction, spheroids were formed by the cells in the 384-well plate, so images of spheroids in each well were captured using Operetta CLS (PerkinElmer) according to a high-content screening method. To maintain the spheroid form of the cells in each well, washing was not performed before analysis. The captured images were converted into volume through additional analysis, and the spheroid volume values by concentration were standardized based on the spheroid treated with the lowest concentration of drug. Graphs were created with a log (inhibitor) vs. normalized response - Variable slope using GraphPad Prism 9.3.1, and IC5 o values were obtained.

   Click to Show/Hide
In Vitro Model lung cancer AMB-LC-0003T cells Homo sapiens
References
Ref 1 Anti-ror1 antibodies and their uses