Linker Information

General Information of This Linker
Linker ID
LIN0DOFAU
Linker Name
N-Methoxycarbonylmaleimide
Antibody-Linker Relation
Uncleavable
Structure
Formula
C6H5NO4
Isosmiles
COC(=O)N1C(=O)C=CC1=O
PubChem CID
580610
InChI
InChI=1S/C6H5NO4/c1-11-6(10)7-4(8)2-3-5(7)9/h2-3H,1H3
InChIKey
LLAZQXZGAVBLRX-UHFFFAOYSA-N
IUPAC Name
methyl 2,5-dioxopyrrole-1-carboxylate
Pharmaceutical Properties
Molecule Weight
155.11
Polar area
63.7
Complexity
237
xlogp Value
-0.3
Heavy Count
11
Rot Bonds
1
Hbond acc
4
Hbond Donor
0
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Neolymphostin ADC 24 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
195 nM
High HER2 expression (HER2+++)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
202 nM
High HER2 expression (HER2+++)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
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)
216 nM
Moderate HER2 expression (HER2++)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Breast adenocarcinoma MDA-MB-361 cells CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 750 nM Negative HER2 expression (HER2-)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
References
Ref 1 Novel PIKK inhibitor antibody-drug conjugates: Synthesis and anti-tumor activity. Bioorg Med Chem Lett. 2019 Apr 1;29(7):943-947. doi: 10.1016/j.bmcl.2019.01.009. Epub 2019 Jan 11.

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