vantictumab   Click here for help

GtoPdb Ligand ID: 10197

Compound class: Antibody
Comment: Vantictumab (OMP-18R5) is an anti-FZD antagonistic monoclonal that induces inhibition of the Wnt signalling pathway [2]. It is being developed by OncoMed Pharmaceuticals. As receptors for Wnt ligands the FZD receptors are molecular targets for the prevention and treatment of cancer and inflammation that lie upstream of β‑catenin. Inhibition of Wnt-induced FZD activation by vantictumab reduces tumour cell proliferation and in vivo tumorigenicity [1], indicating the potential utility of blocking the activation of selected members of the FZD receptor family as a treatment for a wide range of tumours.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
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Bioactivity Comments
Vantictumab binds to 5 of the 10 human FZD receptors; FZD1, FZD2, FZD5, FZD7 and FZD8 [1]. The IC50 values provided in the table are estimates made from the binding curves produced in [1] and indicate the concentration of vantictumab that inhibits Wnt binding to each FZD receptor by 50%.
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
FZD1 Hs Antibody Antagonist ~9.1 pIC50 - 1
pIC50 ~9.1 (IC50 ~7x10-10 M) [1]
FZD7 Hs Antibody Antagonist ~9.0 pIC50 - 1
pIC50 ~9.0 (IC50 ~1x10-9 M) [1]
FZD2 Hs Antibody Antagonist ~9.0 pIC50 - 1
pIC50 ~9.0 (IC50 ~1.1x10-9 M) [1]
FZD5 Hs Antibody Antagonist ~9.0 pIC50 - 1
pIC50 ~9.0 (IC50 ~1.09x10-9 M) [1]
FZD8 Hs Antibody Antagonist ~8.0 pIC50 - 1
pIC50 ~8.0 (IC50 ~1x10-8 M) [1]