Linker Information

General Information of This Linker

Linker ID	LIN0AZEYN
Linker Name	Sulfatase-responsive linker
Linker Type	Sulfatase-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
Structure	3D MOL	2D MOL
Isosmiles	O=C(N1CCOCC(N=N2)=CN2C3=CC=C(CN(CCNC(OCC4=CC([N+]([O-])=O)=C(O[S-](=O)(=O)=O)C=C4)=O)C(O)=O)C=C3)C=CC1=O

Each Antibody-drug Conjugate Related to This Linker

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

37222285 ADC 1 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.49 nM	Positive HER2 expression (HER2+++/++)
Method Description	Next, the dose dependent cytotoxicity of ADC1 was investigated in HER2-positive (BT474 and SK-BR3) and HER2-negative (MCF-7) breast cancer cell lines. The potency of ADC1 was compared to the FDA approved ADC Kadcyla®. ADC1 proved to be highly potent in both BT474 and SK-BR3 cell lines while having negligible toxicity in MCF-7 cells, indicating neglectable extracellular linker cleavage (Fig. 4). We also observed that ADC 1 had a higher potency against BT-474 cells (IC50 = 0.49 nM) compared to Kadcyla (IC50 =1.06 nM) suggesting efficient intracellular linker cleavage and payload release. Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

References

Ref 1	Targeted delivery of alcohol-containing payloads with antibody-drug conjugates