IGF-1R

Isoform-selective Products

Signaling Pathway

IGF-1R Signaling Pathway

IGF-1R Products

  • All (27)
  • IGF-1R Inhibitors (22)
  • IGF-1R Antagonist (1)
  • IGF-1R Modulators (3)
  • New IGF-1R Products
Catalog 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; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.
Nat Commun, 2024, 15(1):828
Dev Cell, 2024, 59(3):326-338.e5
Mol Syst Biol, 2023, e11510.
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.
Nat Commun, 2024, 15(1):51
iScience, 2024, 27(2):109015.
Clin Cancer Res, 2023, 29(7):1317-1331
S1069 Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Sci Adv, 2024, 10(8):eadk3663
bioRxiv, 2024, 10.1101/2024.01.16.575190
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
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.
Acta Pharm Sin B, 2023, 13(9):3744-3755
Nature, 2022, 604(7905):354-361
Cancer Cell, 2022, S1535-6108(22)00312-9
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.
Mol Neurodegener, 2023, 18(1):31
Cell Rep Med, 2023, 4(9):101162
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101285
S7668 Picropodophyllin (PPP) 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.
Bone Res, 2023, 11(1):20
Cell Rep, 2023, 42(8):112984
Mol Cancer Ther, 2023, 22(1):63-74
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.
J Thorac Oncol, 2023, S1556-0864(23)00797-9
NPJ Precis Oncol, 2023, 7(1):12
J Med Chem, 2023, 66(17):12130-12140
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.
Pharmaceuticals (Basel), 2024, 17(2)197
J Neurooncol, 2023, 162(1):109-118.
PLoS One, 2023, 18(2):e0277308
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.
Cancers -Basel), 2023, 15(19)4772
Cell Discov, 2022, 8(1):95
Nat Commun, 2022, 13(1):6345
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).
EMBO Rep, 2023, 24(7):e56937
Nat Biotechnol, 2022, 10.1038/s41587-022-01386-z
Pharmaceuticals (Basel), 2022, 15(2)241
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; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.
Front Cell Dev Biol, 2023, 11:1142586
Cancers -Basel), 2023, 15(19)4772
Cancer Cell, 2022, S1535-6108(22)00312-9
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.
Sci Signal, 2022, 15(747):eabj5879
Cancer Cell, 2021, S1535-6108(21)00383-4
J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X
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.
Exp Mol Med, 2022, 54(8):1225-1235
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
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.
Breast Cancer Res, 2023, 25(1):84
Kaohsiung J Med Sci, 2023, 10.1002/kjm2.12652
Cancers (Basel), 2022, 14(24)6247
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy.
bioRxiv, 2023, 10.1101/2023.12.19.572304
Burns Trauma, 2020, 8:tkaa025
Cancers (Basel), 2020, 12(9)E2668
S6955New 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.
Discov Oncol, 2023, 14(1):139
Discov Oncol, 2023, 14(1):139
Cell Death Dis, 2022, 13(4):351
S8003 PQ 401 PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
Acta Pharmacol Sin, 2018, 39(12):1894-1901
J Chemother, 2016, 28(1):44-9
Lung Cancer, 2015, 90(2):175-81
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis.
E2459 Ginsenoside Rg5 Ginsenoside Rg5, the main component of Red ginseng, blocks binding of IGF-1 to its receptor with an IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
E3106 Dioscoreae Nipponicae Rhizoma Extract Dioscoreae Nipponicae Rhizoma Extract is extracted from the rhizome of Dioscorea nipponica, of which the main component decreases the phosphorylation in IGF-1R, which in turn inhibits the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and Graves’ disease remission.
E0794 MID-1 MID-1 is a disruptor of MG53-IRS-1 (Mitsugumin 53-insulin receptor substrate-1) interaction, which can disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1 expression level and increased insulin signaling and glucose uptake.
S7453 MSDC-0160 MSDC-0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being studied to treat diabetes and Alzheimer's disease. Phase 2.
E0939 Insulin Degludec Insulin degludec is an acylated basal insulin with a unique mechanism of protracted absorption involving the formation of a depot of soluble multihexamer chains after subcutaneous injection, shows a very long duration of action, with a half-life exceeding 25 h in PK/PD studies.
S6443 Chromium picolinate Chromium picolinate is a coordination complex consisting of chromium(III) and picolinic acid. It is used as a nutritional supplement for optimal insulin function in patients with Type 2 diabetes or promotion of weight loss.
S3187 SBI-477 SBI-477 is an insulin signaling inhibitor that deactivates the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain-containing 4 (ARRDC4). SBI-477 inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
S6922 S961 S961 is a biosynthetic insulin receptor antagonist that inhibits cellular proliferation and colony formation in breast tumour cells.
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively.
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.
Nat Commun, 2024, 15(1):828
Dev Cell, 2024, 59(3):326-338.e5
Mol Syst Biol, 2023, e11510.
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.
Nat Commun, 2024, 15(1):51
iScience, 2024, 27(2):109015.
Clin Cancer Res, 2023, 29(7):1317-1331
S1069 Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Sci Adv, 2024, 10(8):eadk3663
bioRxiv, 2024, 10.1101/2024.01.16.575190
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
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.
Acta Pharm Sin B, 2023, 13(9):3744-3755
Nature, 2022, 604(7905):354-361
Cancer Cell, 2022, S1535-6108(22)00312-9
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.
Mol Neurodegener, 2023, 18(1):31
Cell Rep Med, 2023, 4(9):101162
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101285
S7668 Picropodophyllin (PPP) 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.
Bone Res, 2023, 11(1):20
Cell Rep, 2023, 42(8):112984
Mol Cancer Ther, 2023, 22(1):63-74
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.
J Thorac Oncol, 2023, S1556-0864(23)00797-9
NPJ Precis Oncol, 2023, 7(1):12
J Med Chem, 2023, 66(17):12130-12140
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.
Pharmaceuticals (Basel), 2024, 17(2)197
J Neurooncol, 2023, 162(1):109-118.
PLoS One, 2023, 18(2):e0277308
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.
Cancers -Basel), 2023, 15(19)4772
Cell Discov, 2022, 8(1):95
Nat Commun, 2022, 13(1):6345
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).
EMBO Rep, 2023, 24(7):e56937
Nat Biotechnol, 2022, 10.1038/s41587-022-01386-z
Pharmaceuticals (Basel), 2022, 15(2)241
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; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.
Front Cell Dev Biol, 2023, 11:1142586
Cancers -Basel), 2023, 15(19)4772
Cancer Cell, 2022, S1535-6108(22)00312-9
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.
Sci Signal, 2022, 15(747):eabj5879
Cancer Cell, 2021, S1535-6108(21)00383-4
J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X
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.
Exp Mol Med, 2022, 54(8):1225-1235
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
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.
Breast Cancer Res, 2023, 25(1):84
Kaohsiung J Med Sci, 2023, 10.1002/kjm2.12652
Cancers (Basel), 2022, 14(24)6247
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy.
bioRxiv, 2023, 10.1101/2023.12.19.572304
Burns Trauma, 2020, 8:tkaa025
Cancers (Basel), 2020, 12(9)E2668
S8003 PQ 401 PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
Acta Pharmacol Sin, 2018, 39(12):1894-1901
J Chemother, 2016, 28(1):44-9
Lung Cancer, 2015, 90(2):175-81
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis.
E2459 Ginsenoside Rg5 Ginsenoside Rg5, the main component of Red ginseng, blocks binding of IGF-1 to its receptor with an IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
E3106 Dioscoreae Nipponicae Rhizoma Extract Dioscoreae Nipponicae Rhizoma Extract is extracted from the rhizome of Dioscorea nipponica, of which the main component decreases the phosphorylation in IGF-1R, which in turn inhibits the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and Graves’ disease remission.
E0794 MID-1 MID-1 is a disruptor of MG53-IRS-1 (Mitsugumin 53-insulin receptor substrate-1) interaction, which can disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1 expression level and increased insulin signaling and glucose uptake.
S3187 SBI-477 SBI-477 is an insulin signaling inhibitor that deactivates the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain-containing 4 (ARRDC4). SBI-477 inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively.
S6922 S961 S961 is a biosynthetic insulin receptor antagonist that inhibits cellular proliferation and colony formation in breast tumour cells.
S6955New 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.
Discov Oncol, 2023, 14(1):139
Discov Oncol, 2023, 14(1):139
Cell Death Dis, 2022, 13(4):351
S7453 MSDC-0160 MSDC-0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being studied to treat diabetes and Alzheimer's disease. Phase 2.
E0939 Insulin Degludec Insulin degludec is an acylated basal insulin with a unique mechanism of protracted absorption involving the formation of a depot of soluble multihexamer chains after subcutaneous injection, shows a very long duration of action, with a half-life exceeding 25 h in PK/PD studies.
S6955New 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.
Discov Oncol, 2023, 14(1):139
Discov Oncol, 2023, 14(1):139
Cell Death Dis, 2022, 13(4):351

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Tags: IGF-1R pathway | IGF-1R cancer | IGF-1R signaling | IGF-1R pathway | IGF-1R phosphorylation | IGF-1 receptor signaling | IGF-1R signaling pathway | IGF-1 receptor signaling pathway | IGF-1R inhibitor review