Linker Information

General Information of This Linker
Linker ID
LIN0JQEEP
Linker Name
Maleamic methyl ester-based linker 12C
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C28H42N6O8
Isosmiles
CC(C)C(NC(=O)CCCCCNC(=O)/C=C\C(=O)O)C(=O)NC(CCCNC(N)=O)C(=O)Nc1ccc(CO)cc1
InChI
InChI=1S/C28H42N6O8/c1-18(2)25(34-23(37)8-4-3-5-15-30-22(36)13-14-24(38)39)27(41)33-21(7-6-16-31-28(29)42)26(40)32-20-11-9-19(17-35)10-12-20/h9-14,18,21,25,35H,3-8,15-17H2,1-2H3,(H,30,36)(H,32,40)(H,33,41)(H,34,37)(H,38,39)(H3,29,31,42)/b14-13-
InChIKey
HCHVAPGDNXTNOV-YPKPFQOOSA-N
Pharmaceutical Properties
Molecule Weight
590.678
Polar area
229.05
Complexity
42
xlogp Value
0.5089
Heavy Count
42
Rot Bonds
19
Hbond acc
7
Hbond Donor
8
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Mil40-12C [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)
0.06 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)
0.10 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)
0.24 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)
12.71 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
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
20.07 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
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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