General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0TLDLT
ADC Name
TWEAKR ADC 3c
Synonyms
TWEAKR-ADC-3c
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 4 Indication(s)
Bladder cancer [ICD11:2C94]
Investigative
Colon cancer [ICD11:2B90]
Investigative
Lung mucoepidermoid carcinoma [ICD11:2C25]
Investigative
Pancreatic ductal adenocarcinoma [ICD11:2C10]
Investigative
Drug-to-Antibody Ratio
3.7
Antibody Name
BAY-356
 Antibody Info 
Antigen Name
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
 Antigen Info 
Payload Name
Kinesin spindle protein (KSP) inhibitor 3c
 Payload Info 
Therapeutic Target
Kinesin-like protein KIF11 (KIF11)
 Target Info 
Linker Name
Open-chain glycine maleimide
 Linker Info 
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 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.3
nM
LoVo cells
Colon adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.8
nM
NCI-H292 cells
Lung mucoepidermoid carcinoma
Half Maximal Inhibitory Concentration (IC50) 
2.1
nM
BxPC-3 cells
Pancreatic ductal 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 (IC50) 0.30 nM Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Colon adenocarcinoma LoVo cells CVCL_0399
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.80 nM Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 2.10 nM Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
References
Ref 1 Antibody-Prodrug Conjugates with KSP Inhibitors and Legumain-Mediated Metabolite Formation. Chemistry. 2019 Jun 21;25(35):8208-8213. doi: 10.1002/chem.201900441. Epub 2019 Apr 15.

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