Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0QJKGD
ADC Name	Trastuzumab-PC4AP-DOX
Synonyms	Trastuzumab PC4AP DOX Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
Drug-to-Antibody Ratio	2
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Doxorubicin		Payload Info
Therapeutic Target	DNA topoisomerase 2-alpha (TOP2A)		Target Info
Linker Name	Photocaged C4AP		Linker Info
Conjugate Type	Random conjugation through reduced inter-chain cysteines.

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)	203	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 1000	nM	MCF-7 cells	Invasive breast carcinoma

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)	203 nM	Positive HER2 expression (HER2 +++/++)
Method Description	SK-BR-3 cells were incubated with 500 nM of trastuzumab and 39 respectively for 30 min at rt, followed by incubation After washing 3 times with PBS, cells were stained with DAPI (300 uL, 10 ug/mL) at rt for 7 min.
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)	> 1000 nM	Negative HER2 expression (HER2 -)
Method Description	MCF7 cells were incubated with 500 nM of trastuzumab and 39 respectively for 30 min at rt, followed by incubation After washing 3 times with PBS, cells were stained with DAPI (300 uL, 10 ug/mL) at rt for 7 min.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

References

Ref 1	A light-responsive, self-immolative linker for controlled drug delivery via peptide- and protein-drug conjugates. Chem Sci. 2019 Aug 19;10(39):8973-8980. doi: 10.1039/c9sc03016f. eCollection 2019 Oct 21.