General Information of This Linker
Linker ID
LIN0YWQKT
Linker Name
Dansylcadaverine deglycosylated-BCN based linker
Linker Type
Bioorthogonal reaction linker
Antibody-Linker Relation
Cleavable
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Trastuzumab deglycosylated WT-MMAE [Investigative]
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)
0.12 nM
Positive HER2 expression (HER2+++/++)
Method Description
Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative HER2 expression (HER2 -)
Method Description
Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
References
Ref 1 Tag-free, specific conjugation of glycosylated IgG1 antibodies using microbial transglutaminase. RSC Adv. 2022 Nov 22;12(52):33510-33515. doi: 10.1039/d2ra05630e. eCollection 2022 Nov 22.
Ref 2 Hiding Payload Inside the IgG Fc Cavity Significantly Enhances the Therapeutic Index of Antibody-Drug Conjugates. J Med Chem. 2023 Jan 12;66(1):1011-1026. doi: 10.1021/acs.jmedchem.2c01812. Epub 2022 Dec 30.

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