Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0WKDIB
ADC Name
38283215 ADC 25
Synonyms
ADC 25
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Organization
AbbVie Bioresearch Center; WuXi AppTec.
Drug Status
Investigative
Drug-to-Antibody Ratio
3.4
Structure
Antibody Name
undisclosed
Antigen Name
Tumor necrosis factor (TNF)
  Antigen Info 
Payload Name
GRM payload C1
  Payload Info 
Linker Name
Val-Glu linker
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteine.
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 Effective Concentration (EC50) 
0.79
ug/mL
CVCL_0004
Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia
Half Maximal Effective Concentration (EC50) 
> 50
ug/mL
CVCL_0004
Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia
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 Effective Concentration (EC50) 0.79 ug/mL High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

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In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

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In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
References
Ref 1 Impact of dipeptide on ADC physicochemical properties and efficacy identifies Ala-Ala as the optimal dipeptide