General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0QKALQ
ADC Name
H- (A114C)-#58
Synonyms
H- (A114C)-#58
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Organization
PFIZER INC.
Drug Status
Investigative
Drug-to-Antibody Ratio
2
Structure
Antibody Name
anti-CD33-11A1-v1417- (K290C)- (K334C) and CD33-11A1-v1417- (K334C)- (K392C) mAb
 Antibody Info 
Antigen Name
Myeloid cell surface antigen CD33 (CD33)
 Antigen Info 
Payload Name
H- (A114C)-#30 Payload
 Payload Info 
Linker Name
H- (A114C)-#43 Linker
 Linker Info 
Conjugate Type
114C
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 (lC50) 
734
ng/mL
CVCL_0620
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
1433
ng/mL
CVCL_0179
Invasive breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
> 60000
ng/mL
CVCL_0320
Colon 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 (lC50) 734 ng/mL Positive Her2 expression (Her2+++/++)
Method Description
Her2-Target expressing MDA-MB-361-DYT2 (breast cancer) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 45 concentrations.
In Vitro Model Breast adenocarcinoma MDA-MB-361-DYT2 cells CVCL_0620
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 1433 ng/mL Positive Her2 expression (Her2+++/++)
Method Description
Her2-Target expressing (BT474 (breast cancer), N87 (gastric cancer), MDA-MB-361-DYT2 (breast cancer)) or Her2-non-expressing (MDA-MB-468, HT29) cells, or CD33-target expressing HL60, HEL92.1.7, NB4 or CD33-non-expressing (Raji) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 45 concentrations.

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In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 60000 ng/mL Negative Her2 expression (Her2-)
Method Description
Her2-non-expressing HT29) cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 31 concentrations.
In Vitro Model Colon adenocarcinoma HT29 cells (HER2-) CVCL_0320
References
Ref 1 Heteroaryl sulfone-based conjugation handles, methods for their preparation, and their use in synthesizing antibody drug conjugates