1. Protein Tyrosine Kinase/RTK
  2. IGF-1R

IGF-1R

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.

IGF-1R Related Products (43):

Cat. No. Product Name Effect Purity
  • HY-10191
    Linsitinib Inhibitor 99.83%
    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[1].
  • HY-15494
    Picropodophyllin Inhibitor 99.90%
    Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
  • HY-10200
    BMS-754807 Inhibitor 99.71%
    BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively[1].
  • HY-13020
    GSK1838705A Inhibitor 98.95%
    GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.
  • HY-15656
    Ceritinib Inhibitor 99.97%
    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[1][2].
  • HY-P99712
    Lonigutamab Inhibitor
    Lonigutamab (hz208F2-4) is a humanized anti-IGF-1R monoclonal antibody that can be used for the synthesis of antibody–drug conjugates (ADC)[1].
  • HY-P99672
    Istiratumab Inhibitor
    Istiratumab (M-6495) is bispecific monoclonal antibody targeting IGF-1R and ErbB3. Istiratumab induces IGF-1R and ErbB3 receptor degradation through the proteasome pathway Istiratumab can be used for research of cancers[1][2][3].
  • HY-P99713
    Lonigutamab ugodotin Inhibitor
    Lonigutamab ugodotin (W0101) is a humanized IgG1κ monoclonal antibody targeting to IGF-1R. Lonigutamab ugodotin can be used in ADCs preparation. Lonigutamab ugodotin induces tumor regression in breast cancer models with IGF-1R overexpression without affecting normal cells[1][2].
  • HY-N0908
    Ginsenoside Rg5 Agonist
    Ginsenoside Rg5 is the main component of Red ginseng. Ginsenoside blocks binding of IGF-1 to its receptor with an IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
  • HY-13686
    PQ401 Inhibitor 99.85%
    PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis[1].
  • HY-15609
    AZD-3463 Inhibitor 99.96%
    AZD-3463 (ALK/IGF1R inhibitor) is an orally active ALK/IGF1R inhibitor, with a Ki of 0.75 nM for ALK. AZD3463 induces apoptosis and autophagy in neuroblastoma cells[1][2][3].
  • 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[1].
  • 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].
  • 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.
  • HY-110135A
    NBI-31772 hydrate Inhibitor
    NBI-31772 hydrate is a potent inhibitor of interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). NBI-31772 hydrate is also a nonpeptide ligand that releases bioactive IGF-I from the IGF-I/IGFBP-3 complex (Kis=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects[1][2][3].
  • HY-15656S
    Ceritinib D7 Inhibitor
    Ceritinib-d7 is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor[1].
  • 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[1][2][3].
  • HY-18785
    Indirubin Derivative E804 Inhibitor 99.79%
    Indirubin Derivative E804 is a potent inhibitor of Insulin-like Growth Factor 1 Receptor (IGF1R), with an IC50 of 0.65 μM for IGF1R.
  • HY-P99197
    Figitumumab Inhibitor
    Figitumumab (CP-751871) is a potent and fully human monoclonal anti–insulin-like growth factor 1 receptor (IGF1R) antibody. Figitumumab prevents IGF1 from binding to IGF1R with an IC50 of 1.8 nM[1].
  • HY-110135
    NBI-31772 Inhibitor 98.99%
    NBI-31772 is the potent and nonselective inhibitor of IGFBP with a Ki value of 47 nM. NBI-31772 has the potential for the research of IGF-responsive diseases[1].