Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0JDRZK
ADC Name	hCD46-26
Synonyms	hCD46 26 Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Uterine sarcoma [ICD11:2C72] Investigative
	3D MOL	2D MOL
Antibody Name	Anti-CD46 mAb		Antibody Info
Antigen Name	Membrane cofactor protein (CD46)		Antigen Info
Payload Name	PNU-159682		Payload Info
Therapeutic Target	DNA topoisomerase 2-alpha (TOP2A)		Target Info
Linker Name	Maleimide based noncleavable linker 26		Linker Info

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)	0.1	nM	MES-SA cells	Uterine sarcoma
Half Maximal Effective Concentration (EC50)	0.19	nM	HEK293T cells	Normal

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)	0.10 nM	Positive CD46 expression (CD46 +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Uterine sarcoma	MES-SA cells		CVCL_1404
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 nM	Positive CD46 expression (CD46 +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Normal	HEK293T cells		CVCL_0063

References

Ref 1	Evaluation of PNU-159682 antibody drug conjugates (ADCs). Bioorg Med Chem Lett. 2020 Dec 15;30(24):127640. doi: 10.1016/j.bmcl.2020.127640. Epub 2020 Oct 28.