| S6922 |
S961 |
S961 is a biosynthetic insulin receptor antagonist that inhibits cellular proliferation and colony formation in breast tumour cells. |
Selective |
|
| 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. |
Selective |
Insulin Receptor, IC50: 1.6 nM |
| S1124 |
BMS-754807 |
BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met (c-Met), Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2. |
Selective |
Insulin Receptor, IC50: 1.7 nM |
| S7083 |
Ceritinib |
Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3. |
Selective |
Insulin Receptor, IC50: 7 nM |
| S4967 |
Ceritinib dihydrochloride |
Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitomor activity. |
Selective |
InsR, IC50: 7 nM |
| S1093 |
GSK1904529A |
GSK1904529A (GSK 4529) is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM in cell-free assays, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc. |
Selective |
Insulin Receptor, IC50: 25 nM |
| S1012 |
BMS-536924 |
BMS-536924 (CS-0117) 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. |
Selective |
Insulin Receptor, IC50: 73 nM |
| S1091 |
Linsitinib (OSI-906) |
Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3. |
Selective |
Insulin Receptor, IC50: 75 nM |
| S1034 |
NVP-AEW541 |
NVP-AEW541 is a potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM in cell-free assays, greater potency and selectivity for IGF-1R in a cell-based assay. |
Selective |
Insulin Receptor, IC50: 0.14 μM |
| S8229 |
Brigatinib |
Brigatinib is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy. |
Selective |
InsR, IC50: 196 nM |
| S1234 |
AG-1024 |
AG-1024 (Tyrphostin, AGS 200) 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). |
Selective |
Insulin Receptor, IC50: 57 μM |
