Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0FQFDY
ADC Name	Trastuzumab-SG3227
Synonyms	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	2.22
Structure
	3D MOL	2D MOL
Antibody Name	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	Partial reduction of the trastuzumab inter-chain disulfide bonds to release cysteine thiols, then react with the iodoacetamide-containing payload.
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)	1.48	ng/mL	NCI-N87 cells	Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	2130	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)	1.48 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxic effect of Trastuzumab-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 Trastuzumab-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)	2130.00 ng/mL	Negative expression (HER2-)
Method Description	The cytotoxic effect of Trastuzumab-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 Trastuzumab-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.