General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0LQSMZ
ADC Name
CLL1-5 ADC
Synonyms
CLL1 5 ADC; CLL1-5-ADC
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Drug Status
Investigative
Indication
In total 2 Indication(s)
Acute myeloid leukaemia [ICD11:2A60]
Investigative
Chronic eosinophilic leukaemia [ICD11:2A20]
Investigative
Drug-to-Antibody Ratio
6
Antibody Name
Anti-CLL1 mAb
 Antibody Info 
Antigen Name
C-C motif chemokine 1 (CCL1)
 Antigen Info 
Payload Name
GNE-987 (R)
 Payload Info 
Therapeutic Target
Bromodomain-containing protein 4 (BRD4)
 Target Info 
Linker Name
Dolaflexin polymer
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 8 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 27.7
%
EoL-1 cells
Chronic eosinophilic leukemia
Tumor Growth Inhibition value (TGI) 
≈ 48.81
%
HL-60 cells
Adult acute myeloid leukemia
Tumor Growth Inhibition value (TGI) 
≈ 61.2
%
EoL-1 cells
Chronic eosinophilic leukemia
Tumor Growth Inhibition value (TGI) 
≈ 71.08
%
HL-60 cells
Adult acute myeloid leukemia
Tumor Growth Inhibition value (TGI) 
≈ 79.2
%
EoL-1 cells
Chronic eosinophilic leukemia
Tumor Growth Inhibition value (TGI) 
≈ 89.2
%
EoL-1 cells
Chronic eosinophilic leukemia
Tumor Growth Inhibition value (TGI) 
≈ 93.89
%
HL-60 cells
Adult acute myeloid leukemia
Tumor Growth Inhibition value (TGI) 
≈ 100
%
HL-60 cells
Adult acute myeloid leukemia
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 27.70% (Day 6) High CCL1 expression (CCL1 +++)
Method Description
Single intravenous (IV) administration of the CLL1-5 ADC to mice bearing EOL-1 AML xenografts, each conjugate (in 0.5 mg/kg) that were administered once IV at the day 0 time point.
In Vivo Model EOL-1 CDX model
In Vitro Model Chronic eosinophilic leukemia EoL-1 cells CVCL_0258
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 48.81% (Day 10) High CCL1 expression (CCL1 +++)
Method Description
Single intravenous (IV) administration of the CLL1-5 ADC to mice bearing HL-60 AML xenografts, each conjugate (in 0.5 mg/kg) that were administered once IV at the day 0 time point.
In Vivo Model HL-60 CDX model
In Vitro Model Adult acute myeloid leukemia HL-60 cells CVCL_0002
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 61.20% (Day 6) High CCL1 expression (CCL1 +++)
Method Description
Single intravenous (IV) administration of the CLL1-5 ADC to mice bearing EOL-1 AML xenografts, each conjugate (in 1.5 mg/kg) that were administered once IV at the day 0 time point.
In Vivo Model EOL-1 CDX model
In Vitro Model Chronic eosinophilic leukemia EoL-1 cells CVCL_0258
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 71.08% (Day 10) High CCL1 expression (CCL1 +++)
Method Description
Single intravenous (IV) administration of the CLL1-5 ADC to mice bearing HL-60 AML xenografts, each conjugate (in 1.5 mg/kg) that were administered once IV at the day 0 time point.
In Vivo Model HL-60 CDX model
In Vitro Model Adult acute myeloid leukemia HL-60 cells CVCL_0002
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 79.20% (Day 6) High CCL1 expression (CCL1 +++)
Method Description
Single intravenous (IV) administration of the CLL1-5 ADC to mice bearing EOL-1 AML xenografts, each conjugate (in 5 mg/kg) that were administered once IV at the day 0 time point.
In Vivo Model EOL-1 CDX model
In Vitro Model Chronic eosinophilic leukemia EoL-1 cells CVCL_0258
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 89.20% (Day 6) High CCL1 expression (CCL1 +++)
Method Description
Single intravenous (IV) administration of the CLL1-5 ADC to mice bearing EOL-1 AML xenografts, each conjugate (in 10 mg/kg) that were administered once IV at the day 0 time point.
In Vivo Model EOL-1 CDX model
In Vitro Model Chronic eosinophilic leukemia EoL-1 cells CVCL_0258
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93.89% (Day 10) High CCL1 expression (CCL1 +++)
Method Description
Single intravenous (IV) administration of the CLL1-5 ADC to mice bearing HL-60 AML xenografts, each conjugate (in 5 mg/kg) that were administered once IV at the day 0 time point.
In Vivo Model HL-60 CDX model
In Vitro Model Adult acute myeloid leukemia HL-60 cells CVCL_0002
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 10) High CCL1 expression (CCL1 +++)
Method Description
Single intravenous (IV) administration of the CLL1-5 ADC to mice bearing HL-60 AML xenografts, each conjugate (in 10 mg/kg) that were administered once IV at the day 0 time point.
In Vivo Model HL-60 CDX model
In Vitro Model Adult acute myeloid leukemia HL-60 cells CVCL_0002
References
Ref 1 Antibody Conjugation of a Chimeric BET Degrader Enables in?vivo Activity. ChemMedChem. 2020 Jan 7;15(1):17-25. doi: 10.1002/cmdc.201900497. Epub 2019 Nov 14.

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