| S7668 |
Picropodophyllin (PPP) |
Picropodophyllin (PPP) is a selective IGF-1R inhibitor with IC50 of 1 nM. Phase 1/2.
|
Selective |
IGF-1R, IC50: 1 nM |
| S1088 |
NVP-ADW742 |
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 |
| S8003 |
PQ 401 |
PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM. |
Selective |
IGF-1R, IC50: <1 μM |
| S1124 |
BMS-754807 |
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 |
| S2703 |
GSK1838705A |
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 |
| S1093 |
GSK1904529A |
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 |
| S1091 |
OSI-906 (Linsitinib) |
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 |
| S1012 |
BMS-536924 |
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 |
| S1034 |
NVP-AEW541 |
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 |
| S1234 |
AG-1024 |
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 |