Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0VPOLY
ADC Name	Trastuzumab-iCME
Synonyms	Trastuzumab iCME Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Membrane-impermable colchinolmethyl ether (iCME) cytotoxin		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Pacific blue fluorophore-SH based linker		Linker Info
Conjugate Type	Random conjugation through nucleophilic lysines

General Information of The Activity Data Related to This ADC

Revealed Based on the Cell Line Data

Click To Hide/Show 3 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	0.11	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	7.00±5.00	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	14.00±8.00	nM	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 3 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM±0.07 nM	Positive HER2 expression (HER2 +++/++)
Method Description	To quantify cellular cytotoxicity, dose-response curves were generated with HER2-positive SKBR3 cells and HER2-negative MDA-MB-468 cells after treating with ADC and cholesterol-linked endosome-disruptive peptide (Chol-EDP) for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 nM±5.00 nM	Positive HER2 expression (HER2 +++/++)
Method Description	To quantify cellular cytotoxicity, dose-response curves were generated with HER2-positive SKBR3 cells and HER2-negative MDA-MB-468 cells after treating with ADC for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 nM±8.00 nM	Negative HER2 expression (HER2 -)
Method Description	To quantify cellular cytotoxicity, dose-response curves were generated with HER2-positive SKBR3 cells and HER2-negative MDA-MB-468 cells after treatment for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

References

Ref 1	Antibody-Drug Conjugate that Exhibits Synergistic Cytotoxicity with an Endosome-Disruptive Peptide. ACS Omega. 2019 Jul 31;4(7):12955-12968. doi: 10.1021/acsomega.9b01585. eCollection 2019 Jul 31.