General Information of This Linker
Linker ID
LIN0CPZVG
Linker Name
3-Maleimidopropionic acid linker
Linker Type
Uncleavable linker
Antibody-Linker Relation
Uncleavable
Structure
Formula
C7H7NO4
Isosmiles
O=C(N1CCC(O)=O)C=CC1=O
InChI
InChI=1S/C7H7NO4/c9-5-1-2-6(10)8(5)4-3-7(11)12/h1-2H,3-4H2,(H,11,12)
InChIKey
IUTPJBLLJJNPAJ-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
169.136
Polar area
74.68
Complexity
235.2118756
xlogp Value
-0.6139
Heavy Count
12
Rot Bonds
3
Hbond acc
3
Hbond Donor
1
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
US20250025567A1 ExL1A1 [Investigative]
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 lnhibition value (TGl) > 50% Positive CLDN6 expression (CLDN6+++/++)
Method Description
ExL1A1 was tested in SCID mice that subcutaneously transplanted NUGC33, 3 mg/kg was administeredthrough the tail vein of the tumor-bearing mice.
In Vivo Model NUGC-3 cells SCID mice model
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data The ADC concentration required to produce 10,000 pg/mL TNF-alpha was evaluated.
100- 1000 nM
Positive CLDN6 expression (CLDN6+++/++)
Method Description
ExL1A1 was tested in co-culture system consisting of Human peripheral blood mononuclear cells (PBMCs) and NUGC33 cells, with the concentration range of 5.5 uM to 0.97 uM,TNF-a and INF-y productions were measured.
In Vitro Model Normal; Gastric adenocarcinoma PBMC cells; NUGC3 cells .;CVCL_1612
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data The ADC concentration required to produce 10,000 pg/mL INF-Gamma was evaluated.
10- 100 nM
Positive CLDN6 expression (CLDN6+++/++)
Method Description
ExL1A1 was tested in co-culture system consisting of Human peripheral blood mononuclear cells (PBMCs) and NUGC33 cells, with the concentration range of 5.5 uM to 0.97 uM,TNF-a and INF-y productions were measured.
In Vitro Model Normal; Gastric adenocarcinoma PBMC cells; NUGC3 cells .;CVCL_1612
US20250025567A1 ExL7A1 [Investigative]
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 lnhibition value (TGl) > 50% Positive CLDN6 expression (CLDN6+++/++)
Method Description
ExL7A1 was tested in SCID mice that subcutaneously transplanted NUGC33, 3 mg/kg was administeredthrough the tail vein of the tumor-bearing mice.
In Vivo Model NUGC-3 cells SCID mice model
US20250025567A1 ExL1A2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data The ADC concentration required to produce 10,000 pg/mL TNF-alpha was evaluated. > 1000 nM Positive CLDN6 expression (CLDN6+++/++)
Method Description
ExL1A2 was tested in co-culture system consisting of Human peripheral blood mononuclear cells (PBMCs) and NUGC33 cells, with the concentration range of 5.5 uM to 0.97 uM,TNF-a and INF-y productions were measured.
In Vitro Model Normal; Gastric adenocarcinoma PBMC cells; NUGC3 cells .;CVCL_1612
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data The ADC concentration required to produce 10,000 pg/mL INF-Gamma was evaluated.
100- 1000 nM
Positive CLDN6 expression (CLDN6+++/++)
Method Description
ExL1A2 was tested in co-culture system consisting of Human peripheral blood mononuclear cells (PBMCs) and NUGC33 cells, with the concentration range of 5.5 uM to 0.97 uM,TNF-a and INF-y productions were measured.
In Vitro Model Normal; Gastric adenocarcinoma PBMC cells; NUGC3 cells .;CVCL_1612
References
Ref 1 Antibody-drug complex containing Toll-like receptor 7/8 dual agonist compound