Linker Information

General Information of This Linker
Linker ID
LIN0EPTLV
Linker Name
Maleamic methyl ester-based Val-Ala-PABC linker 12a
Linker Type
Thiol-sensitive 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 biosimilar mil40 12a [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 nM
Positive HER2 expression (HER2 +++/++)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
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)
0.05 nM
Positive HER2 expression (HER2 +++/++)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
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)
0.09 nM
Positive HER2 expression (HER2 +++/++)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.22 nM
Positive HER2 expression (HER2 +++/++)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
23.31 nM
Negative HER2 expression (HER2 -)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
24.14 nM
Negative HER2 expression (HER2 -)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
References
Ref 1 Development of applicable thiol-linked antibody-drug conjugates with improved stability and therapeutic index. Drug Deliv. 2022 Dec;29(1):754-766. doi: 10.1080/10717544.2022.2039807.

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