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IGF-1R

The insulin-like growth factor 1 (IGF-1) receptor is a protein found on the surface of human cells. It is a transmembrane receptor that is activated by a hormone called insulin-like growth factor 1 (IGF-1) and by a related hormone called IGF-2. It belongs to the large class of tyrosine kinase receptors. This receptor mediates the effects of IGF-1, which is a polypeptide protein hormone similar in molecular structure to insulin. IGF-1 plays an important role in growth and continues to have anabolic effects in adults – meaning that it can induce hypertrophy of skeletal muscle and other target tissues. Mice lacking the IGF-1 receptor die late in development, and show a dramatic reduction in body mass, testifying to the strong growth-promoting effect of this receptor.

  • Insulin (human)
    T822111061-68-0
    Insulin (human) is a peptide hormone that promotes glycogen synthesis and regulates glucose levels in the blood. Insulin (human) has hypoglycemic activity and is used clinically to treat hyperglycemia in diabetic patients.
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  • GSK1904529A
    T60031089283-49-7In house
    GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .
    • $34
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  • Ceritinib
    T17911032900-25-6
    Ceritinib (LDK378) is a specific ALK inhibitor (IC50: 0.2 nM).
    • $45
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  • GIP (human) acetate
    TP2018L
    GIP (human) acetate is a stimulator of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. GIP (human) acetate plays a vital role in lipid metabolism and the development of obesity.
    • $238
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  • WAY-270250
    T77624852367-46-5
    WAY-270250 is an IGF-1R/SRC inhibitor.
    • $37
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  • Lenaldekar
    T24398418800-15-4
    Lenaldekar (LDK) inhibits T-cell expansion and autoimmune encephalomyelitis. Lenaldekar causes dephosphorylation of members of the PI3 kinase AKT mTOR pathway and delays sensitive cells in late mitosis.
    • $148
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  • Xenin 8 acetate
    TP2209L
    Xenin 8 acetate is a biologically active fragment of Xenin in the neurotensin/xenopsin family. Xenin 8 acetate augments Arginine-induced insulin release (by 40%) and potentiates the glucagon responses to both Arginine (by 60%), Carbachol (by 50%).
    • $243
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  • GIP (1-30) amide, porcine acetate
    T37588L
    GIP (1-30) amide, porcine acetate is an agonist of fully glucose-dependent insulinotropic polypeptide (GIP) receptor. GIP (1-30) amide, porcine acetate can weakly inhibit gastric acid secretion and strongly stimulate insulin.
    • $79
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  • PQ401 hydrochloride (196868-63-0(free base))
    T4324
    PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
    • $37
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  • AZ7550 hydrochloride
    T13564L2309762-40-9
    AZ7550 hydrochloride (AZ7550 hydrochloride ), an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).
    • $126
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  • KW-2450 free base
    T68405904899-25-8In house
    KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.
    • $588
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  • HNMPA
    T21761132541-52-7In house
    HNMPA is a membrane impermeable inhibitor of insulin receptor tyrosine kinase. HNMPA inhibits tyrosine and serine autophosphorylation by the human insulin receptor. HNMPA exhibits no effect on cyclic AMP-dependent protein kinase or protein kinase C activities.
    • $43
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  • Tyrphostin AG 538
    T67707133550-18-2In house
    Tyrphostin AG 538 is a chalcone compound, an IGF-1 receptor kinase inhibitor (IC₅0 : for 400 nM) that is potent, cell-permeable, reversible, and competitive.
    • $100
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  • I-OMe-Tyrphostin AG 538
    T115931094048-77-7In house
    I-OMe-Tyrphostin AG 538 is a specific IGF-1R inhibitor and ATP-competitive inhibitor of PI5P4Kα (IC50: 1 µM).I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and exhibits preferential cytotoxicity to nutrient-deficient PANC1 cells.
    • $51
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  • Rhoifolin
    T275517306-46-6
    Rhoifolin (Apigenin 7-O-neohesperidoside) is extracted from Turpinia arguya Seem dried leaves.
    • $120
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  • NVP-AEW541
    T6080475489-16-8
    NVP-AEW541 (AEW541), a potent inhibitor of IGF-1R(IC50=150 nM) and InsR(IC50=140 nM), exhibits excellent efficiency and specificity for IGF-1R in a cell-based assay.
    • $41
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  • MSDC 0160
    T2607146062-49-9
    MSDC 0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being used in trials studying the treatment of Type 2 Diabetes and Alzheimer's Disease.
    • $30
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  • NVP-TAE 226
    T1918761437-28-9
    NVP-TAE 226 (TAE226) is an effective FAK inhibitor (IC50: 5.5 nM) and most effective to Pyk2(IC50: 3.5 nM); 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.
    • $41
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  • Linsitinib
    T6017867160-71-2
    OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.
    • $33
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  • Urolithin C
    TN7108165393-06-6
    Urolithin C is a gut metabolite of ellagic acid. Urolithin C induces apoptosis in PC12 cells through a mitochondria-mediated pathway.
    • $48
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  • NT157
    T46051384426-12-3
    NT157 is a small molecule tyrphostin targeting IRS protein and has the potential to inhibit IGF-1R and STAT3 signaling pathways in TME cancer cells and stromal cells, resulting in decreased cancer cell survival.
    • $50
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  • Picropodophyllin
    T6943477-47-4
    Picropodophyllin (Picropodophyllin (PPP)) (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast stem cell growth factor (KIT).
    • $58
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  • Brigatinib
    T36211197953-54-0
    Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor.
    • $30
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  • PD173074
    T2642219580-11-7
    PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.
    • $36
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  • GIP (3-42), human
    T375891802086-25-4
    GIP (3-42), human (Gastric Inhibitory Polypeptide (3-42) (human)) is a peptide that acts as a glucose-dependent proinsulinotropic polypeptide (GIP) receptor antagonist and regulates insulin secretion and the metabolic effects of GIP in vivo, which can be used to study type 2 diabetes.
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  • Xentuzumab
    T767951417158-65-6
    Xentuzumab (BI836845) is a recombinant monoclonal antibody to humanised IGF ligand that inhibits IGF1 and IGF2 growth-promoting signalling and inhibits AKT activation for the study of solid tumours.
    • $347
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  • Dusigitumab
    T806051204390-13-5
    Dusigitumab (MEDI 573) is a human IgG2λ monoclonal antibody targeting the insulin-like growth factors IGF2 and IGF1, offering therapeutic potential for conditions related to these proteins [1].
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  • Veligrotug
    T808712728655-31-8
    Veligrotug is a chimeric monoclonal antibody of the IgG1-kappa class that targets the insulin-like growth factor 1 receptor (IGF1R, CD221) [1].
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  • GIP (3-42), human acetate
    T37589L
    GIP (3-42), human acetate is an antagonist of a glucose-dependent insulinotropic polypeptide (GIP) receptor and regulates insulin secretion and GIP metabolism in vivo.
    • $227
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  • MID-1
    T8773312608-54-1
    MID-1 is an inhibitor of MG53-IRS-1 (Mitsugumin 53-Insulin Receptor Substrate-1) interaction. It 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
    • $76
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  • Chromeceptin
    T60055331859-86-0
    Chromeceptin is an inhibitor of the IGF signaling pathway, decreases the numbers of tumorsphere, and inhibits the AKT/mTOR pathway.
    • $31
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  • Insulin(cattle)
    TP112511070-73-8
    Insulin bovine (Insulin from bovine pancreas) is a biologically derived two-chain polypeptide hormone, synthesized in vivo by pancreatic β cells. It is frequently utilized as a growth supplement in cell culture applications.
    • $48
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  • AGL-2263
    T14142638213-98-6
    AGL-2263 is a blocker of insulin receptor (IR)
      7-10 days
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    • Serpentine
      TN499718786-24-8
      Serpentine is an alkaloid found in the roots of Rosa Centifolia that acts as an insulin sensitizer to assist insulin in lowering blood glucose.Serpentine activates the phosphorylation of AMPK, which stimulates glucose uptake by C2C12 cells.Serpentine increases the expression of GSK-3β mRNA in muscle tissues, which enhances glucose uptake.Serpentine also increases glucose production and hepatic gluconeogenesis.Serpentine has a significant effect on glucagon secretion and hepatic gluconeogenesis. Serpentine significantly increased glucagon secretion and hepatic gluconeogenesis. In high-fat diet/streptozotocin (HFD/STZ)-induced diabetic mice, Serpentine significantly prolonged insulin hypoglycemia, significantly decreased exogenous insulin use, and inhibited endogenous insulin secretion.
      • $465
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    • ALK inhibitor 1
      T10285761436-81-1
      ALK inhibitor 1 is a selective ALK kinase inhibitor.
      • $80
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    • NBI-31772
      T8906374620-70-9
      NBI-31772 (NBI 31772) is the potent inhibitor of insulin-like growth factor-1 binding protein (IGFBP, Ki = 47 nM). NBI-31772 can be used in research on IGF-responsive diseases.
      • $51
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    • Picropodophyllotoxin
      T3S002717434-18-3
      Picropodophyllotoxin (AXL 1717) is a cyclolignan alkaloid found in the mayapple plant family (Podophyllum peltatum), and a small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF1R) with potential antineoplastic activity. Picropodophyllotoxin (AXL 1717) specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT). This agent shows potent activity in the suppression o f tumor cell proliferation and the induction of tumor cell apoptosis. IGF1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a critical role in the growth and survival of many types of cancer cells.
      • $32
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    • Ceritinib dihydrochloride
      T1791L1380575-43-8
      Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive inhibitor of ALK tyrosine kinase(IC50 of 200 pM), and also inhibits IGF-1R, InsR, and STK22D (IC50 values of 8, 7, and 23 nM, respectively), shows great antitumor potency
      • $43
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    • GSK1838705A
      T30791116235-97-2
      GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases.
      • $34
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    • AG1024
      T269365678-07-1
      AG1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM).
      • $34
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    • NVP-ADW742
      T6079475488-23-4
      NVP-ADW742 (ADW) 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.
      • $48
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    • AZD-3463
      T19671356962-20-3
      AZD-3463 (ALK/IGF1R inhibitor) , an orally bioavailable ALK inhibitor (Ki: 0.75 nM), can inhibit IGF1R with equivalent potency.
      • $48
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    • PQ401
      T2085196868-63-0
      PQ401 (IGF-1R Inhibitor II) suppresses autophosphorylation of IGF-1R domain(IC50<1 μM).
      • $63
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    • BMS-754807
      T23491001350-96-4
      Dual IGF-1R/InsR Inhibitor BMS-754807 is an oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity.
      • $45
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    • AVJ16
      T9980
      AVJ16 as a member of the insulin growth factor 2 mRNA-binding protein family, binds to the mRNA of certain genes to regulate protein translation.
      • $139
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    • Ginsenoside Rg5
      T6S1487186763-78-0
      1. Ginsenoside Rg5 could be a beneficial agent for the treatment of Alzheimer's disease. 2. Ginsenoside Rg5 suppresses LPS-induced nitric oxide (NO) production and proinflammatory TNF-α secretion. 3. Ginsenoside Rg5 can ameliorate lung inflammation possib
      • $115
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    • URMC-099
      T60571229582-33-5
      URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
      • $52
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    • XL228
      T17267898280-07-4
      XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).
      • $51
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    • PD168393
      T6932194423-15-9
      PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.
      • $33
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    • AZ7550
      T135641421373-99-0
      AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).
      • $133
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