Linker Information

General Information of This Linker
Linker ID
LIN0WTVJH
Linker Name
Mal-PEG4
Antibody-Linker Relation
Uncleavable
Structure
Formula
C18H24N2O10
Isosmiles
C1CC(=O)N(C1=O)OC(=O)COCCOCCOCCOCCN2C(=O)C=CC2=O
PubChem CID
154730904
InChI
InChI=1S/C18H24N2O10/c21-14-1-2-15(22)19(14)5-6-26-7-8-27-9-10-28-11-12-29-13-18(25)30-20-16(23)3-4-17(20)24/h1-2H,3-13H2
InChIKey
GMCIZYRLSCHXJA-UHFFFAOYSA-N
IUPAC Name
(2,5-dioxopyrrolidin-1-yl) 2-[2-[2-[2-[2-(2,5-dioxopyrrol-1-yl)ethoxy]ethoxy]ethoxy]ethoxy]acetate
Pharmaceutical Properties
Molecule Weight
428.4
Polar area
138
Complexity
644
xlogp Value
-2.1
Heavy Count
30
Rot Bonds
16
Hbond acc
10
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
Tb085-SG3376 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
9.00 pM
Method Description
On day 3, groups of five mice were then treated with (1) 0.25 mg/kg Tb085-SG3376 or (2) 0.25 mg/kg NIP228-SG3376 or (3) PBS alone. Three uninfected mice were used as negative controls for the BLI.
In Vitro Model . T. brucei gambiense (T. b. brucei) .
FOLR1-Mal-PEG4-Eribulin [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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.28 nM
High FOLR1 expression(FOLR1+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Ovarian endometrioid adenocarcinoma IGROV-1 cells CVCL_1304
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
22.00 nM
Moderate FOLR1 expression(FOLR1++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Lung non-small cell carcinoma NCI-H2110 cells CVCL_1530
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Low FOLR1 expression(FOLR1+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative FOLR1 expression(FOLR1-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma SJSA-1 cells CVCL_1697
MSLN-Mal-PEG4-Eribulin [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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
32.00 nM
Moderate MSLN expression(MSLN++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Lung non-small cell carcinoma NCI-H2110 cells CVCL_1530
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
76.00 nM
Negative MSLN expression(MSLN-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Ovarian endometrioid adenocarcinoma IGROV-1 cells CVCL_1304
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative MSLN expression(MSLN-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative MSLN expression(MSLN-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma SJSA-1 cells CVCL_1697
References
Ref 1 A single dose of antibody-drug conjugate cures a stage 1 model of African trypanosomiasis. PLoS Negl Trop Dis. 2019 May 23;13(5):e0007373. doi: 10.1371/journal.pntd.0007373. eCollection 2019 May.
Ref 2 MORAb-202, an Antibody-Drug Conjugate Utilizing Humanized Anti-human FR Farletuzumab and the Microtubule-targeting Agent Eribulin, has Potent Antitumor Activity. Mol Cancer Ther. 2018 Dec;17(12):2665-2675. doi: 10.1158/1535-7163.MCT-17-1215. Epub 2018 Sep 27.

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