General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0XXPBB
ADC Name
wO2024105206A1 3k-2658
Synonyms
WO2024105206A1 3k-2658
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Organization
VINCERX PHARMA GMBH
Drug Status
Investigative
Drug-to-Antibody Ratio
4.1
Structure
Antibody Name
TPP-2658
 Antibody Info 
Antigen Name
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
 Antigen Info 
Payload Name
Ac-Exatecan
 Payload Info 
Therapeutic Target
DNA topoisomerase I (TOP1)
 Target Info 
Linker Name
32p-Avelu Linker
 Linker Info 
Conjugate Type
Lysine cuopling
Combination Type
Intermediate Q3
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
13&#459.9
nM
CVCL_1051
Renal cell carcinoma
Half Maximal inhibitory Concentration (lC50) 
103&#4599
nM
CVCL_A8EZ
Colon cancer
Half Maximal inhibitory Concentration (lC50) 
1003&#45999
nM
CVCL_1051
Renal cell carcinoma
Half Maximal inhibitory Concentration (lC50) 
1003&#45999
nM
CVCL_A8EZ
Colon cancer
Activity Concentration at -50% (AC50) 
1.0- 9.9
nM
CVCL_1051
Renal cell carcinoma
Activity Concentration at -50% (AC50) 
10- 99
nM
CVCL_1051
Renal cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
13&#459.9 nM
Method Description
The cells were cultivated according to the standard method using the growth media suggest by provider The test was carried out by detaching the cells with a solution of Accutase in PBS buffer (fromBiochrom AG #L2143).
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
103&#4599 nM
Method Description
The cells were cultivated according to the standard method using the growth media suggest by provider The test was carried out by detaching the cells with a solution of Accutase in PBS buffer (fromBiochrom AG #L2143).
In Vitro Model Colon cancer HT29 cells CVCL_A8EZ
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1003&#45999 nM
Method Description
The cells were cultivated according to the standard method using the growth media suggest by provider The test was carried out by detaching the cells with a solution of Accutase in PBS buffer (fromBiochrom AG #L2143).
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1003&#45999 nM
Method Description
The cells were cultivated according to the standard method using the growth media suggest by provider The test was carried out by detaching the cells with a solution of Accutase in PBS buffer (fromBiochrom AG #L2143).
In Vitro Model Colon cancer HT29 cells CVCL_A8EZ
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 10 % carbon dioxide.

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In Vitro Model Renal cell carcinoma 786-O cells (+NE) CVCL_1051
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 10 % carbon dioxide.

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In Vitro Model Renal cell carcinoma 786-O cells (-NE) CVCL_1051
References
Ref 1 Antibody-drug conjugates cleavable in a tumor microenvironment