Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0QDNEX
ADC Name	CLL1-6 ADC
Synonyms	CLL1 6 ADC; CLL1-6-ADC Click to Show/Hide
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
	3D MOL	2D MOL
Antibody Name	Anti-CLL1 mAb		Antibody Info
Antigen Name	C-C motif chemokine 1 (CCL1)		Antigen Info
Payload Name	GNE-987 (S)		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 3 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 3.1	%	HL-60 cells	Adult acute myeloid leukemia
Tumor Growth Inhibition value (TGI)	≈ 17.24	%	HL-60 cells	Adult acute myeloid leukemia
Tumor Growth Inhibition value (TGI)	≈ 34.8	%	EoL-1 cells	Chronic eosinophilic leukemia

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 3 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 3.10% (Day 11)	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 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 17.24% (Day 11)	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
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.80% (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

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.