Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0RWTUE
ADC Name	hCD46-29
Synonyms	hCD46 29 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	PNU-thiazole cleavable linker 29		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)	41	pM	MES-SA cells	Uterine sarcoma
Half Maximal Effective Concentration (EC50)	1.6	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)	41.00 pM	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)	1.60 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.