Linker Information

General Information of This Linker
Linker ID
LIN0CVLIT
Linker Name
Maleamic methyl ester-based linker 12B
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C25H36N4O7
Isosmiles
CC(NC(=O)C(NC(=O)CCCCCNC(=O)/C=C\C(=O)O)C(C)C)C(=O)Nc1ccc(CO)cc1
InChI
InChI=1S/C25H36N4O7/c1-16(2)23(29-21(32)7-5-4-6-14-26-20(31)12-13-22(33)34)25(36)27-17(3)24(35)28-19-10-8-18(15-30)9-11-19/h8-13,16-17,23,30H,4-7,14-15H2,1-3H3,(H,26,31)(H,27,36)(H,28,35)(H,29,32)(H,33,34)/b13-12-
InChIKey
VDHDDXNCUKYMKX-SEYXRHQNSA-N
Pharmaceutical Properties
Molecule Weight
504.584
Polar area
173.93
Complexity
36
xlogp Value
1.0803
Heavy Count
36
Rot Bonds
15
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
Mil40-12B [Investigative]
 ADC Info 
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) ≈ 80.00% (Day 60) High HER2 expression (HER2+++)
Method Description
Mil40-12b induces efficient tumor cell killing in cell PDX models from a breast cancer patient with HER2 expression.
In Vivo Model Breast ductal carcinoma CDX model
In Vitro Model Breast ductal carcinoma Breast ductal carcinoma cells Homo sapiens
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)
25.80 pM
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 (3x104 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)
53.60 pM
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 (3x104 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)
102.60 pM
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 (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)
207.40 pM
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 (3x104 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)
11.52 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)
26.44 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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