Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0LEQIY
ADC Name	Mu-Alpha-EGFR-172
Synonyms	Mu-alpha-EGFR 172 Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Melanoma [ICD11:2C30] Investigative
Drug-to-Antibody Ratio	4
Structure
	3D MOL	2D MOL
Antibody Name	mu-alpha-EGFR		Antibody Info
Antigen Name	Epidermal growth factor receptor (EGFR)		Antigen Info
Payload Name	IMSA172		Payload Info
Therapeutic Target	Stimulator of interferon genes protein (STING1)		Target Info
Linker Name	Mc-Val-Cit-PABC		Linker Info
Conjugate Type	A mutant version of cetuximab hu-alphaEGFR(ACVC), provides four cysteines (heavy chain A114C and light chain V205C)on each antibody and was used for site-specific conjugation.

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 Inhibitory Concentration (IC50)	1.3	nM	THP1-Lucia ISG cells	Acute monocytic leukemia
Half Maximal Inhibitory Concentration (IC50)	> 10	uM	THP1-Lucia ISG cells	Acute monocytic leukemia

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 Inhibitory Concentration (IC50)	1.30 nM	High EGFR expression (EGFR+++)
Method Description	Serial dilutions of IMSA172 or its conjugates with the indicated antibodies (ADCs) were incubated with THP1-ISG-Luc or this cell line stably expressing human EGFR (THP1-ISG-luc-EGFR; B and D) for 16 h, and the interferon response was measured by luciferase assay.
In Vitro Model	Acute monocytic leukemia	THP1-Lucia ISG cells		CVCL_X587
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	Negative EGFR expression (EGFR-)
Method Description	Serial dilutions of IMSA172 or its conjugates with the indicated antibodies (ADCs) were incubated with THP1-ISG-Luc or this cell line stably expressing human EGFR (THP1-ISG-luc-EGFR; B and D) for 16 h, and the interferon response was measured by luciferase assay.
In Vitro Model	Acute monocytic leukemia	THP1-Lucia ISG cells		CVCL_X587

References

Ref 1	Tumor-targeted delivery of a STING agonist improvescancer immunotherapy. Proc Natl Acad Sci U S A. 2022 Dec 6;119(49):e2214278119.