| S1091 |
Linsitinib (OSI-906)
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Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays. It is modestly potent to InsR with IC50 of 75 nM, and shows no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.
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Nat Commun, 2025, 16(1):2493
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Cell Rep Med, 2025, 6(8):102297
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Cell Rep Med, 2025, 6(8):102254
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| S1012 |
BMS-536924
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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.
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Leukemia, 2025, 39(4):917-928
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MedComm (2020), 2024, 5(12):e70033
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Cancers -Basel), 2023, 15(19)4772
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| S1034 |
NVP-AEW541
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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.
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Acta Pharm Sin B, 2023, 13(9):3744-3755
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Acta Pharm Sin B, 2023, 13(9):3744-3755
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Nature, 2022, 604(7905):354-361
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| S1124 |
BMS-754807
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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.
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Cell Rep, 2025, 44(8):116149
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Commun Med (Lond), 2025, 5(1):206
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Front Cell Neurosci, 2024, 18:1441827
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| S7668 |
Picropodophyllin (AXL1717)
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Picropodophyllin (PPP, AXL1717) is a IGF-1R inhibitor with IC50 of 1 nM. It displays selectivity for IGF-1R and does not coinhibit tyrosine phosphorylation the IR, or of a selected panel of receptors less related to IGF-IR(FGF-R, PDGF-R, OR EGF-R). Picropodophyllin (PPP) induces apoptosis with antineoplastic activity.
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Cell Rep Med, 2025, 6(2):101927
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Small Sci, 2025, 5(12):e202500140
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Cell Rep, 2025, 44(8):116149
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| S1093 |
GSK1904529A
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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.
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Pharmaceuticals (Basel), 2024, 17(2)197
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J Neurooncol, 2023, 162(1):109-118.
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PLoS One, 2023, 18(2):e0277308
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| S1234 |
AG-1024
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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).
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Cells, 2024, 13(14)1222
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EMBO Rep, 2023, 24(7):e56937
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Nat Biotechnol, 2022, 10.1038/s41587-022-01386-z
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| S1088 |
NVP-ADW742
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NVP-ADW742 (GSK 552602A) is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; this compound shows little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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Front Cell Dev Biol, 2023, 11:1142586
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Cancers -Basel), 2023, 15(19)4772
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| S8228 |
NT157
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NT157, a selective inhibitor of IRS-1/2(insulin receptor substrate), has the potential to inhibit IGF-1R and STAT3 signaling pathways in cancer cells and stroma cells of TME leading to a decrease in cancer cell survival.
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Int J Cancer, 2025, 10.1002/ijc.35458
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Eur J Cell Biol, 2024, 103(4):151457
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Int J Biochem Cell Biol, 2024, 176:106676
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| S8003 |
PQ 401
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PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
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Acta Pharmacol Sin, 2018, 39(12):1894-1901
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J Chemother, 2016, 28(1):44-9
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Lung Cancer, 2015, 90(2):175-81
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