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IGF-1R

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IGF-1R Signaling Pathway Map

Isoform-selective Inhibitors

Insulin Receptor Selective

IGF-1R Products

All (23)
IGF-1R Inhibitors (19)
IGF-1R Antagonist (1)
IGF-1R Modulators (3)
New IGF-1R Products

Catalog No.	Product Name	Information	Product Use Citations
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.	Elife, 2022, 11e76183 Oral Dis, 2021, 27(2):290-300 Mol Neurobiol, 2020, 57(3):1570-1593
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.	Toxicol In Vitro, 2022, 83:105384 Cancer Cell, 2021, S1535-6108(21)00383-4 Cancer Cell, 2021, S1535-6108(21)00492-X
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.	Biomedicines, 2022, 10(3)624 Cell Death Discov, 2022, 8(1):86 Cell Rep, 2021, 34(11):108870
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.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Head Neck, 2022, 44(5):1192-1205 Cancer Biomark, 2021, 10.3233/CBM-210016
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, 2022, 13(1):684 Nat Commun, 2022, 13(1):2500 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
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.	Biomolecules, 2022, 12(4)563 Life Sci, 2021, 270:118980 Biol Reprod, 2020, 102(1):116-132
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).	Pharmaceuticals (Basel), 2022, 15(2)241 PLoS One, 2021, 16(2):e0247190 J Hematol Oncol, 2020, 13(1):77
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.
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.	Cancer Res, 2022, 82(2):307-319 NPJ Precis Oncol, 2022, 6(1):11 Nature, 2021, 600(7888):319-323
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.	Cancer Res, 2022, 82(2):307-319 NPJ Precis Oncol, 2022, 6(1):11 Sci Rep, 2022, 12(1):6345
S7106	AZD3463	AZD3463 is a novel orally bioavailable ALK inhibitor with K_i 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.	Ann Neurol, 2022, 10.1002/ana.26383 Cell Rep, 2022, 39(1):110608 Transl Lung Cancer Res, 2022, 11(4):543-559
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.	NPJ Precis Oncol, 2022, 6(1):11 NPJ Precis Oncol, 2022, 6(1):5 Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
S6922	S961	S961 is a biosynthetic insulin receptor antagonist that inhibits cellular proliferation and colony formation in breast tumour cells.
E0939^New	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.
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.	Cell Death Dis, 2022, 13(4):351 Biol Pharm Bull, 2022, 45(5):614-624 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.	Elife, 2022, 11e76183 Oral Dis, 2021, 27(2):290-300 Mol Neurobiol, 2020, 57(3):1570-1593
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.	Toxicol In Vitro, 2022, 83:105384 Cancer Cell, 2021, S1535-6108(21)00383-4 Cancer Cell, 2021, S1535-6108(21)00492-X
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.	Biomedicines, 2022, 10(3)624 Cell Death Discov, 2022, 8(1):86 Cell Rep, 2021, 34(11):108870
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.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Head Neck, 2022, 44(5):1192-1205 Cancer Biomark, 2021, 10.3233/CBM-210016
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, 2022, 13(1):684 Nat Commun, 2022, 13(1):2500 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
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.	Biomolecules, 2022, 12(4)563 Life Sci, 2021, 270:118980 Biol Reprod, 2020, 102(1):116-132
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).	Pharmaceuticals (Basel), 2022, 15(2)241 PLoS One, 2021, 16(2):e0247190 J Hematol Oncol, 2020, 13(1):77
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.
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.	Cancer Res, 2022, 82(2):307-319 NPJ Precis Oncol, 2022, 6(1):11 Nature, 2021, 600(7888):319-323
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.	Cancer Res, 2022, 82(2):307-319 NPJ Precis Oncol, 2022, 6(1):11 Sci Rep, 2022, 12(1):6345
S7106	AZD3463	AZD3463 is a novel orally bioavailable ALK inhibitor with K_i 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.	Ann Neurol, 2022, 10.1002/ana.26383 Cell Rep, 2022, 39(1):110608 Transl Lung Cancer Res, 2022, 11(4):543-559
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.	NPJ Precis Oncol, 2022, 6(1):11 NPJ Precis Oncol, 2022, 6(1):5 Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
S6922	S961	S961 is a biosynthetic insulin receptor antagonist that inhibits cellular proliferation and colony formation in breast tumour cells.
E0939^New	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.
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.	Cell Death Dis, 2022, 13(4):351 Biol Pharm Bull, 2022, 45(5):614-624 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.
E0939^New	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.