- Insulin Receptor
IGF-1R Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
Picropodophyllin (PPP) is a selective IGF-1R inhibitor with IC50 of 1 nM. Phase 1/2.
|Selective||IGF-1R, IC50: 1 nM|
NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.
|Selective||IGF-1R, IC50: 0.17 μM|
PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
|Selective||IGF-1R, IC50: <1 μM|
BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.
|Pan||IGF-1R, IC50: 1.8 nM|
GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.
|Pan||IGF-1R, IC50: 2 nM|
GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.
|Pan||IGF-1R, IC50: 27 nM|
OSI-906 (Linsitinib) is a selective inhibitor of IGF-1R with IC50 of 35 nM; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.
|Pan||IGF-1R, IC50: 35 nM|
BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.
|Pan||IGF-1R, IC50: 100 nM|
NVP-AEW541 is a potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM, greater potency and selectivity for IGF-1R in a cell-based assay.
|Pan||IGF-1R, IC50: 0.15 μM|
AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, is less potent to IR with IC50 of 57 μM and specifically distinguishes between InsR and IGF-1R (as compared to other tyrphostins).
|Pan||IGF-1R, IC50: 7 μM|
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