Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0PTXBI
ADC Name	Hu-Alpha-EGFR (ACVC)-172
Synonyms	Hu-alpha-EGFR (ACVC) 172 Click to Show/Hide
Drug Status	Investigative
Indication	In total 5 Indication(s) Acute granulocytic leukaemia [ICD11:2B33] Clinical candidate Gastrointestinal interstitial cancer [ICD11:2B5B] Clinical candidate Melanoma [ICD11:2C30] Clinical candidate Non-small cell lung cancer [ICD11:2C25] Clinical candidate Small cell lung cancer [ICD11:2C25] Clinical candidate
Drug-to-Antibody Ratio	4
Structure
	3D MOL	2D MOL
Antibody Name	hu-alpha-EGFR(ACVC), cetuximab with A114C and V205C mutations		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)	1.5	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)	1.50 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.