Linker Information

General Information of This Linker

Linker ID	LIN0DLJQE
Linker Name	Tetrazine-PEG5-Val-Ala-PABC
Linker Type	Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
Structure	3D MOL		2D MOL
Formula	C37H52N8O10
Isosmiles	CC(NC(=O)C(NC(=O)CCOCCOCCOCCOCCOCCC(=O)Nc1ccc(-c2nncnn2)cc1)C(C)C)C(=O)Nc1ccc(CO)cc1
InChI	InChI=1S/C37H52N8O10/c1-26(2)34(37(50)40-27(3)36(49)42-31-8-4-28(24-46)5-9-31)43-33(48)13-15-52-17-19-54-21-23-55-22-20-53-18-16-51-14-12-32(47)41-30-10-6-29(7-11-30)35-44-38-25-39-45-35/h4-11,25-27,34,46H,12-24H2,1-3H3,(H,40,50)(H,41,47)(H,42,49)(H,43,48)
InChIKey	RJLYSRPTZAKHPQ-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	768.869	Polar area	234.34
	Complexity	55	xlogp Value	1.5118
	Heavy Count	55	Rot Bonds	27
	Hbond acc	14	Hbond Donor	5

Each Antibody-drug Conjugate Related to This Linker

Full Information of The Activity Data of The ADC(s) Related to This Linker

T-CpHK-Tet-ADC [Investigative]

ADC Info

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)	0.30 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
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)	0.40 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	68.00 nM	Moderate HER2 expression (HER2++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Invasive breast carcinoma	ZR-75-1 cells		CVCL_0588

References

Ref 1	Cyclopentadiene as a Multifunctional Reagent for Normal- and Inverse-Electron Demand Diels-Alder Bioconjugation. Bioconjug Chem. 2022 Sep 21;33(9):1609-1619.