IGF-1R

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IGF-1R Inhibitors (9)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
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, 10.1038/nsmb.2828
  • 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 with IC50 of 86 nM, 27-fold greater selectivity for IGF-1R than InsR.
  • J Clin Invest, 2011, 121(11):4311-21
  • Cancer Discov, 2012, 2(3):227-35
  • Cancer Res, 2011, 71(21):6773-84
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.
  • Cell Death Dis, 2012, 3:e336
  • Exp Gerontol, 2014, 10.1016/j.exger.2014.01.022
  • Oral Dis, 2014, 10.1111/odi.12235
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.
  • Biochem Biophys Res Commun, 2013, 436(4):740-5
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
  • Cell Death Dis, 2012, 3:e336
  • Breast Cancer Res, 2011, 13(3):R52
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.
  • 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
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 1/2.
  • Clin Cancer Res, 2013, 19(11):2984-94