Inhibitor of IGF1R
In Vitro Validations
Uniprot ID: P08069
Target Class: Kinase
Target SubClass: TK
Potency Value: 150 nM
Potency Assay: in vitro kinase assay on isolated kinase domain
PDB ID for probe-target interaction (3D structure): --
Insulin-like growth factor 1 receptor, IGF1R, IGF1 ...
DOI Reference: 10.1016/S1535-6108(04)00051-0
In Cell Validations
In Vivo Data
Off-Target Selectivity Assesments
Potency end-point : IC50 Ins-R 140 nM, TEK 530 nM, FLT1 600 nM, FLT3 420 nM
Potency assay (off target): NVP-AEW541 was at least 10-fold selective for IGF1R over all kinases tested except those listed.
Potency in cells, off target : IC50 Ins-R 2.3 uM
Potency assay, off target (cells): NVP-AEW541 is 27-fold selective for inhibition of IGF1R autophosphorylation > Ins-R autophosphorylation, and had negligible activity against several other tyrosine kinases.
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