General Information of This Linker
Linker ID
LIN0NYNCO
Linker Name
Maleimidocaproyl (Ser3-Gly)3
Linker Type
Nucleotide linker
Antibody-Linker Relation
Uncleavable
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
ADAPT6-ABD-mcDM1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83.30% (Day 23) High HER2 expression (HER2+++)
Method Description
The SKOV3 xenografts were established in female BALB/c nu/nu mice by subcutaneous implantation of 1 x107 SKOV3 cells in 100 uL of medium in the abdominal region. The therapy started one week after the implantation. The mice were randomized in three groups (n = 910). One group of mice received intravenous (i.v.) injections of 13.3 mg/kg of ADAPT6-ABD-mcDM1 in 100 uL of PBS, the second group of mice received i.v. injections of the same dose of ADAPTNeg-ABD-mcDM1 in 100 uL of PBS, and the third group of mice received i.v. injections of 100 uL of PBS.

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In Vivo Model ER2-expressing SKOV3 ovarian cancer xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.00 nM
High HER2 expression (HER2+++)
Method Description
The cytotoxic potential of ADAPT6-ABD-mcDM1 was investigated by incubation of dilution series of the conjugate with cell lines having different HER2-expression levels.
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)
7.00 nM
High HER2 expression (HER2+++)
Method Description
The cytotoxic potential of ADAPT6-ABD-mcDM1 was investigated by incubation of dilution series of the conjugate with cell lines having different HER2-expression levels.
In Vitro Model Breast adenocarcinoma AU565 cells CVCL_1074
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
80.00 nM
High HER2 expression (HER2+++)
Method Description
The cytotoxic potential of ADAPT6-ABD-mcDM1 was investigated by incubation of dilution series of the conjugate with cell lines having different HER2-expression levels.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
References
Ref 1 Experimental HER2-Targeted Therapy Using ADAPT6-ABD-mcDM1 in Mice Bearing SKOV3 Ovarian Cancer Xenografts: Efficacy and Selection of Companion Imaging Counterpart. Pharmaceutics. 2022 Aug 2;14(8):1612.
Ref 2 Targeting HER2 Expressing Tumors with a Potent Drug Conjugate Based on an Albumin Binding Domain-Derived Affinity Protein. Pharmaceutics. 2021 Nov 3;13(11):1847.

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