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IGF-1R Inhibitors (10)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Nat Struct Mol Biol, 2014, 21(6):522-7
  • Blood, 2013, 122(9):1621-33
  • Cancer Res, 2012, 73(2):834-43
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.
  • Cancer Cell, 2015, 27(1):97-108
  • Cancer Discov, 2012, 2(3):227-35
  • J Clin Invest, 2011, 121(11):4311-21
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.
  • Mol Cell Proteomics, 2015, 10.1074/mcp.M114.045468
  • Cell Death Dis, 2012, 3:e336
  • Exp Gerontol, 2014, 52:55-69
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.
  • J Cancer Res Clin Oncol, 2014, 10.1007/s00432-014-1787-z
  • Biochem Biophys Res Commun, 2013, 436(4):740-5
  • UNIVERSITE DE LYON, 2014, Pascal S
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.
  • Clin Cancer Res, 2011, 17(8):2237-49
  • Breast Cancer Res, 2011, 13(3):R52
  • Cancer Prev Res , 2010, 3(10):1222-34
S7668 Picropodophyllin (PPP) Picropodophyllin (PPP) is a selective IGF-1R inhibitor with IC50 of 1 nM. Phase 1/2.
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.
  • Cancer Res, 2014, 74(24):7217-28
  • Mol Cell Proteomics, 2012, 11(6):M112.017764
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).
  • Blood, 2013, 122(9):1621-33
  • J Virol, 89(5):2643-58,
  • Mol Endocrinol, 2011, 25(12):2041-53
S8003 PQ 401 PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <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.
  • Clin Cancer Res, 2013, 19(11):2984-94
  • Mol Cell Biol, 35(7):1182-96,

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