Home Protein Tyrosine Kinase IGF-1R

IGF-1R Inhibitors/Agonists

The insulin-like growth factor (IGF-1 receptor), is a kind of tyrosine kinase receptors activated by IGF-1 is a transmembrane receptor consisting of two alpha-subunits and two transmembrane beta-subunits that are linked by disulfide bonds. The activation of IGF-1 receptors in turn leads to activation of distinct signaling pathways through Grb2, including the phosphatidylinositol 3-kinase (PI3K), Akt pathway and the Ras, Raf, mitogen-activated protein kinase (MAPK) pathway, leading to increasing in proliferation and decreased apoptosis. IGF-1 receptor is implicated in tumor and it is also an attractive target for cancer therapy.

Other Protein Tyrosine Kinase Related Inhibitors

VEGFR EGFR c-Met PDGFR CSF-1R c-Kit ALK Tie-2 HER2 c-RET

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S1091 Linsitinib (OSI-906) 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.
Cancer Biology & Medicine, June 9, 2021, 229-252
Molecular Cancer Therapeutics, January 3, 2023, 63-74
Theranostics, January 1, 2022, 1097-1116
Verified customer review of Linsitinib (OSI-906)
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.
Leukemia, 2025, 39(4):917-928
MedComm (2020), 2024, 5(12):e70033
Cancers -Basel), 2023, 15(19)4772
Verified customer review of BMS-536924
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.
Parasites & Vectors, May 11, 2020, 242
eLife, June 17, 2019, e47061
PLoS One, January 3, 2017, e0169229
Verified customer review of NVP-AEW541
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.
Molecular Cancer Research, September 02 2022, 1405-1419
Acta Pharmacologica Sinica, July 17 2019, 270-277
Cell Reports, August 26 2025, 116149
Verified customer review of BMS-754807
S7668 Picropodophyllin (AXL1717) 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.
Cell Rep Med, 2025, 6(2):101927
Small Sci, 2025, 5(12):e202500140
Cell Rep, 2025, 44(8):116149
Verified customer review of Picropodophyllin (AXL1717)
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).
PLoS Pathogens, 2025, e1013202
Cells, 2024, 13(14)1222
EMBO Rep, 2023, 24(7):e56937
Verified customer review of AG-1024
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.
Acta Pharmaceutica Sinica B, May 2022, 2239-2251
Bioscience Reports, January 30, 2018, BSR20171252
Bioscience Reports, January 30 2018, BSR20171252
Verified customer review of GSK1904529A
S1088 NVP-ADW742 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.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Front Cell Dev Biol, 2023, 11:1142586
Cancers -Basel), 2023, 15(19)4772
Verified customer review of NVP-ADW742
S8228 NT157 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.
Int J Cancer, 2025, 10.1002/ijc.35458
Eur J Cell Biol, 2024, 103(4):151457
Int J Biochem Cell Biol, 2024, 176:106676
S6955 Insulin (human) Insulin (human) (Insulin regular) is a polypeptide hormone that regulates the level of glucose. Insulin is commonly used to treat hyperglycemia in patients with diabetes. Potency: 29 units/mg.
Discover Oncology, July 27, 2023, 14(1):139
Cell & Bioscience, January 17, 2025, 15(1):4
Cell & Bioscience, 2025, 4

Signaling Pathway Map