Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0XIMBQ
ADC Name	Engineered HER-SG3227
Synonyms	Engineered Her-SG3227 Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative Gastric cancer [ICD11:2B72] Investigative
Drug-to-Antibody Ratio	1.68
Structure
	3D MOL	2D MOL
Antibody Name	Engineered trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	SG2219		Payload Info
Therapeutic Target	Human Deoxyribonucleic acid (hDNA)		Target Info
Linker Name	Acetamide-PEG4-Val-Ala-PABA		Linker Info
Conjugate Type	Full reduction followed by re-oxidation of the inter-chain disulfide bonds to selectively free the engineered cysteine thiols for conjugation.
Combination Type	SG3227

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)	4.29	ng/mL	NCI-N87 cells	Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	1220	ng/mL	MDA-MB-468 cells	Breast adenocarcinoma

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)	4.29 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxic effect of Engineered Her-SG3227 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of Engineered Her-SG3227 was assessed on the NCI-N87 cell line.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1220.00 ng/mL	Negative expression (HER2-)
Method Description	The cytotoxic effect of Engineered Her-SG3227 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of Engineered Her-SG3227 was assessed on the MDA-MB-468 cell line.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

References

Ref 1	Synthesis and in vitro evaluation of SG3227, a pyrrolobenzodiazepine dimer antibody-drug conjugate payload based on sibiromycin. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1154-1158.