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

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-135680
    I-OMe-Tyrphostin AG 538
    Inhibitor 98.03%
    I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells.?I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50?of 1 μM.
    I-OMe-Tyrphostin AG 538
  • HY-135436
    AG 538
    Inhibitor 99.80%
    AG 538 is a potent, competitive inhibitor of IGF-1 receptor kinase, with an IC50 of 400 nM.
    AG 538
  • HY-108905
    Mecasermin
    Mecasermin (Human IGF-I; FK 780) is a recombinant human insulin-like growth factor I (IGF-I). Mecasermin has the potential for the study of the growth failure of growth hormone (GH) insensitivity caused by GH receptor defects or GH-inhibiting antibodies.
    Mecasermin
  • HY-15656S
    Ceritinib-d7
    Inhibitor 98.00%
    Ceritinib-d7 is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor[1].
    Ceritinib-d<sub>7</sub>
  • HY-161618
    MJ04
    Inhibitor
    MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg).
    MJ04
  • HY-B0794A
    AZ7550 hydrochloride
    Inhibitor 98.66%
    AZ7550 hydrochloride is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
    AZ7550 hydrochloride
  • HY-156914
    IGF-1R/SRC-IN-1
    Inhibitor 99.86%
    IGF-1R/SRC-IN-1 (Compound 3b) is an inhibitor for IGF-1R (IC50 is 63 μM) and SRC.
    IGF-1R/SRC-IN-1
  • HY-B0794
    AZ7550
    Inhibitor
    AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
    AZ7550
  • HY-125102
    AZ12253801
    Inhibitor
    AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.
    AZ12253801
  • HY-50866B
    NVP-AEW541 dihydrochloride
    Inhibitor
    NVP-AEW541 dihydrochloride (AEW541 dihydrochloride) is an orally active inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with an IC50 value of 0.15 μM. NVP-AEW541 dihydrochloride also inhibits InsR, IC50 with a value of 0.14 μM. NVP-AEW541 dihydrochloride has antitumor activity.
    NVP-AEW541 dihydrochloride
  • HY-100167
    TAK-778
    Agonist
    TAK-778 is a derivative of ipriflavone and has been shown to induce bone growth in in vitro and in vivo models.
    TAK-778
  • HY-B0149R
    Tranexamic acid (Standard)
    Tranexamic acid (Standard) is the analytical standard of Tranexamic acid. This product is intended for research and analytical applications. 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 (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[1][2].
    AZ7550-d<sub>5</sub>
  • HY-P10403
    IGFBP-3 peptide
    IGFBP-3 peptide is a 18-amino acid insulin-like growth factor binding protein-3. IGFBP-3 peptide binds Humanin (HY-P1928) and Hyaluronan (HY-B0633A), blocks the interaction of CD44 and hyaluronan.
    IGFBP-3 peptide
  • HY-135749
    BN201
    Activator
    BN201 promotes neuronal differentiation, the differentiation of precursor cells to mature oligodendrocytes (EC50 of 6.3 μM) in vitro, and the myelination of new axons (EC50 of 16.6 μM). BN201 is able to cross the blood-brain barrier by active transport and activate pathways (IGF-1 pathway) associated with the response to stress and neuron survival. BN201 has potently neuroprotective effects.
    BN201
  • 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-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-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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity