IGF-1R

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IGF-1R Signaling Pathway Map

IGF-1R Signaling Pathways
Isoform-selective Inhibitors

IGF-1R Products

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  • IGF-1R Inhibitors (19)
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  • IGF-1R Modulators (2)
  • New IGF-1R Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
Oral Dis, 2021, 27(2):290-300
Mol Neurobiol, 2020, 57(3):1570-1593
G3 (Bethesda), 2020, 4;10(5):1585-1597
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.
Cancer Cell, 2021, S1535-6108(21)00383-4
Cancer Cell, 2021, S1535-6108(21)00492-X
Development, 2021, 148(7)dev199133
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.
Cell Rep, 2021, 34(11):108870
Haematologica, 2021, 10.3324/haematol.2021.278743
Cancers (Basel), 2021, 13(15)3850
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.
Cancer Biomark, 2021, 10.3233/CBM-210016
Cell Signal, 2020, S0898-6568(20)30362-4
Oncol Rep, 2020, 44(6):2581-2594
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.
Cell Metab, 2021, S1550-4131(21)00326-0
Clin Cancer Res, 2021, 27(9):2533-2548
Theranostics, 2021, 11(4):1918-1936
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.
Life Sci, 2021, 270:118980
Biol Reprod, 2020, 102(1):116-132
Genome Biol, 2020, 21(1):174
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.
Front Oncol, 2021, 11:650052
Life Sci, 2021, 267:118977
Sci China Life Sci, 2021, 10.1007/s11427-020-1836-7
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 One, 2021, 16(2):e0247190
J Hematol Oncol, 2020, 13(1):77
Oncogene, 2019, 38(24):4669-4684
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.
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 Cell, 2021, S1535-6108(21)00383-4
J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X
Cell, 2019, 36(2):179-193
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.
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. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S4967New 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.
Nature, 2021, 600(7888):319-323
Clin Cancer Res, 2021, 27(9):2533-2548
Cancers (Basel), 2021, 13(17)4422
S7083 Ceritinib (LDK378) Ceritinib (LDK378) is 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.
Nature, 2021, 600(7888):319-323
Cell, 2021, 184(10):2649-2664.e18
Clin Cancer Res, 2021, 27(9):2533-2548
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.
Cancers (Basel), 2020, 12(9)E2668
Aging (Albany NY), 2020, 7;12(9):8221-8240
Burns Trauma, 2020, 8:tkaa025
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.
Sci Adv, 2021, 7(27)eabf1068
Cell Rep, 2021, 34(3):108657
Cell Rep, 2021, 34(3):108657
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
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.
Biochim Biophys Acta Mol Cell Res, 2021, 1868(1):118877
PLoS One, 2021, 16(2):e0247190
Technol Cancer Res Treat, 2021, 20:15330338211027916
S8229 Brigatinib (AP26113) Brigatinib (AP26113) 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.
Nature, 2021, 600(7888):319-323
EMBO J, 2021, e105784
Cancer Lett, 2021, 522:119-128
A5188 Insulin Receptor Rabbit Recombinant mAb Insulin Receptor Rabbit Recombinant mAb detects endogenous level of total Insulin Receptor.
S6922 S961 S961 is a biosynthetic insulin receptor antagonist that inhibits cellular proliferation and colony formation in breast tumour cells.
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.
J Virol, 2021, JVI0155021
S7453 MSDC-0160 MSDC-0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being studied to treat diabetes and Alzheimer's disease. Phase 2.
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.
Oral Dis, 2021, 27(2):290-300
Mol Neurobiol, 2020, 57(3):1570-1593
G3 (Bethesda), 2020, 4;10(5):1585-1597
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.
Cancer Cell, 2021, S1535-6108(21)00383-4
Cancer Cell, 2021, S1535-6108(21)00492-X
Development, 2021, 148(7)dev199133
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.
Cell Rep, 2021, 34(11):108870
Haematologica, 2021, 10.3324/haematol.2021.278743
Cancers (Basel), 2021, 13(15)3850
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.
Cancer Biomark, 2021, 10.3233/CBM-210016
Cell Signal, 2020, S0898-6568(20)30362-4
Oncol Rep, 2020, 44(6):2581-2594
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.
Cell Metab, 2021, S1550-4131(21)00326-0
Clin Cancer Res, 2021, 27(9):2533-2548
Theranostics, 2021, 11(4):1918-1936
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.
Life Sci, 2021, 270:118980
Biol Reprod, 2020, 102(1):116-132
Genome Biol, 2020, 21(1):174
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.
Front Oncol, 2021, 11:650052
Life Sci, 2021, 267:118977
Sci China Life Sci, 2021, 10.1007/s11427-020-1836-7
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 One, 2021, 16(2):e0247190
J Hematol Oncol, 2020, 13(1):77
Oncogene, 2019, 38(24):4669-4684
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.
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 Cell, 2021, S1535-6108(21)00383-4
J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X
Cell, 2019, 36(2):179-193
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.
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. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S4967New 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.
Nature, 2021, 600(7888):319-323
Clin Cancer Res, 2021, 27(9):2533-2548
Cancers (Basel), 2021, 13(17)4422
S7083 Ceritinib (LDK378) Ceritinib (LDK378) is 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.
Nature, 2021, 600(7888):319-323
Cell, 2021, 184(10):2649-2664.e18
Clin Cancer Res, 2021, 27(9):2533-2548
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.
Cancers (Basel), 2020, 12(9)E2668
Aging (Albany NY), 2020, 7;12(9):8221-8240
Burns Trauma, 2020, 8:tkaa025
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.
Sci Adv, 2021, 7(27)eabf1068
Cell Rep, 2021, 34(3):108657
Cell Rep, 2021, 34(3):108657
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
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.
Biochim Biophys Acta Mol Cell Res, 2021, 1868(1):118877
PLoS One, 2021, 16(2):e0247190
Technol Cancer Res Treat, 2021, 20:15330338211027916
S8229 Brigatinib (AP26113) Brigatinib (AP26113) 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.
Nature, 2021, 600(7888):319-323
EMBO J, 2021, e105784
Cancer Lett, 2021, 522:119-128
A5188 Insulin Receptor Rabbit Recombinant mAb Insulin Receptor Rabbit Recombinant mAb detects endogenous level of total Insulin Receptor.
S6922 S961 S961 is a biosynthetic insulin receptor antagonist that inhibits cellular proliferation and colony formation in breast tumour cells.
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.
J Virol, 2021, JVI0155021
S7453 MSDC-0160 MSDC-0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being studied to treat diabetes and Alzheimer's disease. Phase 2.
S4967New 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.
Nature, 2021, 600(7888):319-323
Clin Cancer Res, 2021, 27(9):2533-2548
Cancers (Basel), 2021, 13(17)4422
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