IGF-1R Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| 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. |
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| 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. |
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| 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. |
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| S7668 | Picropodophyllin (AXL1717) | Picropodophyllin (PPP, AXL1717) is an IGF-1R inhibitor with an 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. |
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| 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. |
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| 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. |
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| 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). |
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| S1088 | NVP-ADW742 | NVP-ADW742 (GSK 552602A) is an IGF-1R inhibitor with an IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; this compound shows little activity against HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit. |
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| S8228 | NT157 | NT157, a selective inhibitor of IRS-1/2 (insulin receptor substrate), has the potential to inhibit IGF-1R and STAT3 signalling pathways in cancer cells and stroma cells of TME leading to a decrease in cancer cell survival. |
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| S8003 | PQ 401 | PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM. |
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| 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. This compound 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 signalling 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 disrupt molecular association of MG53 with IRS-1 and abolish MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1 expression level and increased insulin signalling and glucose uptake. | ||
| S3187 | SBI-477 | SBI-477 is an insulin signalling 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). This compound inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes. | ||
| S7083 | Ceritinib | Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. This compound also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3. |
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| 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, exhibits weaker potency against the HSP90 family members GRP94 and TRAP-1, and demonstrates the tightest binding of any small-molecule HSP90 ligand. It effectively downregulates and destabilizes the IGF-1Rβ protein, resulting in growth inhibition, autophagy and apoptosis. Phase 2. |
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| 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. |
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| 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 Tyrosine Kinase. |
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| 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. |
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| S7106 | AZD3463 | AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. This compound suppresses cell viability by inducing both cell apoptosis and autophagy. |
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| 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 recognised 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. |
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| E2507 | BI605906 | BI605906 is a selective inhibitor of IKKβ with an IC50 of 380 nM when assayed at 0.1 mM ATP, suppressing the phosphorylation and activation of IKKβ, modulating NF-κB signalling. It also inhibits the insulin-like growth factor 1 (IGF1) receptor, with an IC50 of 7.6 μM. This compound effectively blocks TNF-α-dependent IκB degradation and reduces the expression of proinflammatory cytokines, including IL-6, IL-1β, and C-X-C motif ligands CXCL1/2. | ||
| 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. |
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