Linker Information

General Information of This Linker
Linker ID
LIN0BUDEO
Linker Name
Maleamic methyl ester-based linker 12A
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C22H30N4O7
Isosmiles
CC(NC(=O)C(NC(=O)CCNC(=O)/C=C/C(=O)O)C(C)C)C(=O)Nc1ccc(CO)cc1
InChI
InChI=1S/C22H30N4O7/c1-13(2)20(26-18(29)10-11-23-17(28)8-9-19(30)31)22(33)24-14(3)21(32)25-16-6-4-15(12-27)5-7-16/h4-9,13-14,20,27H,10-12H2,1-3H3,(H,23,28)(H,24,33)(H,25,32)(H,26,29)(H,30,31)/b9-8+
InChIKey
TZBMUWBXXWALDK-CMDGGOBGSA-N
Pharmaceutical Properties
Molecule Weight
462.503
Polar area
173.93
Complexity
33
xlogp Value
-0.09
Heavy Count
33
Rot Bonds
12
Hbond acc
6
Hbond Donor
6
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
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
High HER2 expression (HER2+++)
Method Description
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
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
High HER2 expression (HER2+++)
Method Description
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
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
High HER2 expression (HER2+++)
Method Description
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
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
High HER2 expression (HER2+++)
Method Description
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
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
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
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
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
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.

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