General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0UXODO
ADC Name
EphA2-targeted mAb ADC B 17 (DAR8)
Synonyms
EphA2-targeted-mAb-ADC-B-17-(DAR8)
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Organization
Seagen Inc.
Drug Status
Investigative
Indication
In total 1 Indication(s)
Hodgkin lymphoma [ICD11:2B30]
Investigative
Drug-to-Antibody Ratio
8
Structure
Antibody Name
Brentuximab
 Antibody Info 
Antigen Name
Tumor necrosis factor receptor superfamily member 8 (TNFRSF8)
 Antigen Info 
Payload Name
Undisclosed
Linker Name
EphA2-targeted mAb ADC B 17 (DAR8) linker
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 11 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Effective Concentration (EC50) 
0.2
ng/mL
L540cy cells
Hodgkin's disease
Half Maximal Effective Concentration (EC50) 
1
ng/mL
Karpas-299 cells
ALK-positive anaplastic large cell lymphoma
Half Maximal Effective Concentration (EC50) 
2
ng/mL
MOLM-13 cells
Adult acute myeloid leukemia
Half Maximal Effective Concentration (EC50) 
> 1000
ng/mL
786-O cells
Renal cell carcinoma
Half Maximal Effective Concentration (EC50) 
> 1000
ng/mL
A2058 cells
Melanoma
Half Maximal Effective Concentration (EC50) 
> 1000
ng/mL
BxPC-3 cells
Pancreatic ductal adenocarcinoma
Half Maximal Effective Concentration (EC50) 
> 1000
ng/mL
LS174T cells
Colon adenocarcinoma
Half Maximal Effective Concentration (EC50) 
> 1000
ng/mL
MDA-MB-231 cells
Breast adenocarcinoma
Half Maximal Effective Concentration (EC50) 
> 1000
ng/mL
SU-DHL-4 cells
Diffuse large B-cell lymphoma
Half Maximal Effective Concentration (EC50) 
> 4
pg/mL
DEL cells (Brentuximab vedotin resistant)
Anaplastic large cell lymphoma
Half Maximal Effective Concentration (EC50) 
> 4
pg/mL
DEL cells
Anaplastic large cell lymphoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 11 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.20 ng/mL Positive EPHA2 expression (EPHA2+++/++); Positive CD30 expression (CD30+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the L540cy cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Hodgkin's disease L540cy cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 1.00 ng/mL Positive EPHA2 expression (EPHA2+++/++); Positive CD30 expression (CD30+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the Karpas-299 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 2.00 ng/mL Positive EPHA2 expression (EPHA2+++/++); Negative CD30 expression (CD30-)
Method Description
Potency of compounds and ADCs was evaluated using the MOLM-13 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Adult acute myeloid leukemia MOLM-13 cells CVCL_2119
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 1000 ng/mL Positive EPHA2 expression (EPHA2+++/++); Negative CD30 expression (CD30-)
Method Description
Potency of compounds and ADCs was evaluated using the 786-O cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 1000 ng/mL Positive EPHA2 expression (EPHA2+++/++); Negative CD30 expression (CD30-)
Method Description
Potency of compounds and ADCs was evaluated using the A2058 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Melanoma A2058 cells CVCL_1059
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 1000 ng/mL Positive EPHA2 expression (EPHA2+++/++); Negative CD30 expression (CD30-)
Method Description
Potency of compounds and ADCs was evaluated using the BxPC3 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 1000 ng/mL Positive EPHA2 expression (EPHA2+++/++); Negative CD30 expression (CD30-)
Method Description
Potency of compounds and ADCs was evaluated using the Ls174T cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Colon adenocarcinoma LS174T cells CVCL_1384
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 1000 ng/mL Positive EPHA2 expression (EPHA2+++/++); Negative CD30 expression (CD30-)
Method Description
Potency of compounds and ADCs was evaluated using the MDA-MB-231 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 1000 ng/mL Positive EPHA2 expression (EPHA2+++/++); Negative CD30 expression (CD30-)
Method Description
Potency of compounds and ADCs was evaluated using the SU-DHL-4 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Diffuse large B-cell lymphoma SU-DHL-4 cells CVCL_0539
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 4.00 pg/mL Positive EPHA2 expression (EPHA2+++/++); Positive CD30 expression (CD30+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the DEL cells (Brentuximab vedotin resistance). Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Anaplastic large cell lymphoma DEL cells (Brentuximab vedotin resistant) CVCL_1170
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 4.00 pg/mL Positive EPHA2 expression (EPHA2+++/++); Positive CD30 expression (CD30+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the DEL cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Anaplastic large cell lymphoma DEL cells CVCL_1170
References
Ref 1 Immunomodulatory antibody-drug conjugates; 2022-07-21.

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