General Information of This Linker
Linker ID
LIN0KYENH
Linker Name
Azide-modified dibenzocyclooctyne(DBCO)-albumin(HAS)
Linker Type
Thiol-sensitive 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
P38B-DM1 [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) ≈ 75.00% (Day 18) Positive PDPN expression (PDPN +++/++)
Method Description
One day after cell inoculation, 100 mg of antibodies (P38B-DM1, P38B, or normal canine IgG) in 100 mL of PBS were injected into the peritoneal cavity of each mouse. On days 8 and 14, 5 mg/kg P38B-DM1 was injected into each mouse.
In Vivo Model CHO/dPDPN CDX model
In Vitro Model Melanoma CHO cells (PDPN expression) CVCL_0213
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 48.00 ng/mL Positive PDPN expression (PDPN +++/++)
Method Description
0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
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)
0.09 nM
High HER2 expression (HER2+++)
Method Description
0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.12 nM
High HER2 expression (HER2+++)
Method Description
0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.78 nM
High HER2 expression (HER2+++)
Method Description
0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
35.00 nM
High HER2 expression (HER2+++)
Method Description
0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 6 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
97.62 nM
Low HER2 expression (HER2+)
Method Description
0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 7 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
110.54 nM
Low HER2 expression (HER2+)
Method Description
0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
References
Ref 1 Antibody-Drug Conjugates Using Mouse-Canine Chimeric Anti-Dog Podoplanin Antibody Exerts Antitumor Activity in a Mouse Xenograft Model. Monoclon Antib Immunodiagn Immunother. 2020 Apr;39(2):37-44. doi: 10.1089/mab.2020.0001. Epub 2020 Mar 17.
Ref 2 Antibody-Drug Conjugate Using Ionized Cys-Linker-MMAE as the Potent Payload Shows Optimal Therapeutic Safety. Cancers (Basel). 2020 Mar 21;12(3):744. doi: 10.3390/cancers12030744.

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