1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. IGF-1R

IGF-1R

Insulin-like growth factor-1 receptor

IGF-1R (Insulin-like growth factor 1 receptor), a receptor tyrosine kinase, is activated upon binding to the ligands IGF-1 or IGF-2 leading to cell growth, survival and migration of both normal and cancerous cells.

IGF-1R can initiate the activation of the PI3K/AKT/mTOR signaling and Ras/Raf/MEK/MAPK pathways resulting in the activation of multiple transcription factors such as ELK-1, CREB and AP-1 to modulate cell proliferation, survival, differentiation, motility, invasion and angiogenesis. IGF-1R overexpression or increased IGF-1R kinase activity is associated with a broad range of human cancers and therefore the IGF-1R is widely considered as a very promising target for cancer treatment.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N0908R
    Ginsenoside Rg5 (Standard)
    Agonist
    Ginsenoside Rg5 (Standard) is the analytical standard of Ginsenoside Rg5. This product is intended for research and analytical applications. Ginsenoside Rg5 is the main component of Red ginseng and IGF-1R agonist. Ginsenoside Rg5 compets for the binding site of IGF-1R and blocks the binding of IGF-1 to IGF-1R (IC50 about 90 nM). Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
    Ginsenoside Rg5 (Standard)
  • HY-15494S
    Picropodophyllin-d3
    Picropodophyllin-d3 (AXL1717-d3; Picropodophyllotoxin-d3; PPP-d3) is the deuterium labeled Picropodophyllin (HY-15494). Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
    Picropodophyllin-d<sub>3</sub>
  • HY-P1777A
    IGF-I (24-41) (TFA)
    IGF-I (24-41) (Insulin-like Growth Factor I (24-41)) TFA is amino acids 24 to 41 fragment of IGF-I. IGF-I TFA, a 70 aa polypeptide hormone, is a trophic factor for both neurons and glial cells. IGF-I TFA is partly responsible for systemic growth hormone (GH) activities. IGF-I TFA has anabolic, antioxidant, anti-inflammatory and cytoprotective actions. IGF-I (24-41) TFA regulates somatic growth and behavioral development.
    IGF-I (24-41) (TFA)
  • HY-118046
    GSK2163632A
    Inhibitor
    GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that can be used as a probe for studying heart failure and Parkinson's disease. GSK2163632A potently inhibits GRK1 and GRK5, and also inhibits Rho-associated coiled-coil kinase (ROCK) and insulin-like growth factor receptor IGF-1R. GSK2163632A binds to GRK2 in a manner similar to Paroxetine (HY-122272).
    GSK2163632A
  • HY-P991457
    AVE1642
    Inhibitor
    AVE1642 is a human IgG monoclonal antibody (mAb) targeting CD221/IGF1R. AVE1642 delays growth of tumour xenografts and prolongs the survival of tumour-bearing nude mice. AVE1642 can be used in advanced solid tumours research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
    AVE1642
  • HY-402309
    IGF-1R modulator 1
    Modulator
    IGF-1R modulator 1 (Example 5) is an IGF-1R modulator, with EC50s of 0.29 μM (FGFR1), 0.25 μM (IGF1R), 0.34 μM (TrkA), 0.39 μM (TrkB). IGF-1R modulator 1 can be used for research of diseases characterised by impaired signalling of neurotrophins and/or other trophic factors, such as Alzheimer's disease.
    IGF-1R modulator 1
  • HY-P1773A
    IGF-I (30-41) (TFA)
    IGF-I (30-41) (TFA) is amino acids 30 to 41 fragment of Insulin-like Growth Factor I (IGF-I). IGF-I is partly responsible for systemic GH activities although it possesses a wide number of own properties (anabolic, antioxidant, anti-inflammatory and cytoprotective actions).
    IGF-I (30-41) (TFA)
  • HY-150255
    IMP2-IN-3
    Inhibitor
    IMP2-IN-3 is a potent IMP2 inhibitor. IMP2-IN-3 shows anticancer effects.
    IMP2-IN-3
  • HY-162506
    IGF-1R inhibitor-3
    Inhibitor
    IGF-1R inhibitor-3 (Compound C11) is an allosteric inhibitor for insulin-like growth factor receptor 1 kinase (IGF-1R), with an IC50 of 0.2 μM.
    IGF-1R inhibitor-3
  • HY-169572
    IGF-1R inhibitor-5
    Inhibitor
    IGF-1R inhibitor-5 (compound 19) is a potent inhibitor of IGF-1R, with the IC50 of 6 μM. IGF-1R inhibitor-5 has the potential for the research of cancer.
    IGF-1R inhibitor-5
  • HY-P991134
    Elegrobart
    Inhibitor
    Elegrobart is an immunoglobulin G1-κ monoclonal antibody targeting the human insulin-like growth factor 1 receptor (IGF1R). Elegrobart is promising for research of diseases associated with abnormal IGF1R signaling, especially thyroid eye disease.
    Elegrobart
  • HY-169600
    IGF-1R inhibitor-4
    Inhibitor
    IGF-1R inhibitor-4 (compound 22) is a potent inhibitor of IGF-1R, with the inhibitiron rate of 63% at 10 μM. IGF-1R inhibitor-4 plays an important role in cancer research.
    IGF-1R inhibitor-4
  • HY-15494S1
    Picropodophyllin-d6
    Inhibitor
    Picropodophyllin-d6 (AXL1717-d6) is deuterium labeled Picropodophyllin. Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
    Picropodophyllin-d<sub>6</sub>
  • HY-167854
    KW-2450 free base
    Inhibitor
    KW-2450 Free base is a potent multikinase inhibitor targeting Aurora A and B kinases, demonstrating significant antitumor activity against triple-negative breast cancer (TNBC). KW-2450 Free base effectively reduces cell viability, promotes apoptosis, and inhibits colony formation and mammosphere formation in TNBC cells. KW-2450 Free base significantly suppresses the growth of TNBC xenografts, leading to tetraploid accumulation followed by apoptosis or the survival of octaploid cells. KW-2450 Free base enhances the efficacy of combination therapy with the MEK inhibitor selumetinib, resulting in a synergistic antitumor effect in TNBC models. KW-2450 Free base also acts as an orally bioavailable inhibitor of IGF-1R and IR tyrosine kinases, contributing to its potential antineoplastic activity by inhibiting tumor cell proliferation and inducing apoptosis.
    KW-2450 free base
  • HY-13203R
    NVP-TAE 226 (Standard)
    Inhibitor
    NVP-TAE 226 (Standard) is the analytical standard of NVP-TAE 226. This product is intended for research and analytical applications. NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively.
    NVP-TAE 226 (Standard)
  • HY-15656R
    Ceritinib (Standard)
    Inhibitor 99.72%
    Ceritinib (Standard) is the analytical standard of Ceritinib. This product is intended for research and analytical applications. Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency.
    Ceritinib (Standard)
  • HY-B0149S2
    Tranexamic acid-13C6
    Tranexamic acid-13C6 (Cyclocapron-13C6) is 13C labeled Tranexamic acid. Tranexamic acid (cyclocapron), a cyclic analog of lysine, is an orally active antifibrinolytic agent. Tranexamic acid attenuates the effects of severe trauma, inhibits urokinase plasminogen activator and ameliorates dry wrinkles. Tranexamic acid can used for the research of hemostasis .
    Tranexamic acid-<sup>13</sup>C<sub>6</sub>
  • HY-10191R
    Linsitinib (Standard)
    Inhibitor
    Linsitinib (Standard) is the analytical standard of Linsitinib. This product is intended for research and analytical applications. Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively.
    Linsitinib (Standard)
  • HY-B0794S
    AZ7550-d5
    Inhibitor
    AZ7550-d5 is the deuterium labeled AZ7550?(HY-B0794). AZ7550, an active metabolite of Osimtinib (AZD9291; HY-15772), inhibits the activity of?IGF1R?with an?IC50?of 1.6 μM.
    AZ7550-d<sub>5</sub>
  • HY-110135R
    NBI-31772 (Standard)
    Inhibitor
    NBI-31772 (Standard) is the analytical standard of NBI-31772. This product is intended for research and analytical applications. NBI-31772 is a non-selective IGFBP inhibitor (Ki=47 nM). NBI-31772 has neuroprotective effects and reduces infarct volume during cerebral ischemia. NBI-31772 can also restore or enhance proteoglycan synthesis in osteoarticular chondrocytes. In addition, NBI-31772 also increases the effect of IGF3 on zebrafish oocyte maturation.
    NBI-31772 (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity