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-15656
    Ceritinib
    Inhibitor 99.98%
    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
  • 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.
    Linsitinib
  • 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.
    Picropodophyllin
  • HY-10200
    BMS-754807
    Inhibitor 99.41%
    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.
    BMS-754807
  • HY-13020
    GSK1838705A
    Inhibitor 99.14%
    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.
    GSK1838705A
  • 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-P99867
    Dusigitumab
    Dusigitumab (MEDI 573) is a human IgG2λ monoclonal antibody that specifically targets IGF2 and IGF1.
    Dusigitumab
  • HY-P990084
    Veligrotug
    Inhibitor
    Veligrotug is an IgG1-kappa, anti-IGF1R (insulin-like growth factor 1 receptor, CD221) chimeric monoclonal antibody.
    Veligrotug
  • HY-B0149
    Tranexamic acid
    ≥98.0%
    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
  • HY-50866
    NVP-AEW541
    Inhibitor ≥99.0%
    NVP-AEW541 (AEW541 ) 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 also inhibits InsR, IC50 with a value of 0.14 μM. NVP-AEW541 has antitumor activity.
    NVP-AEW541
  • HY-10262
    BMS-536924
    Inhibitor 99.83%
    BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity.
    BMS-536924
  • HY-15656A
    Ceritinib dihydrochloride
    Inhibitor 99.57%
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency.
    Ceritinib dihydrochloride
  • HY-15609
    AZD-3463
    Inhibitor 99.58%
    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.
    AZD-3463
  • HY-P99294
    Ganitumab
    Inhibitor
    Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer.
    Ganitumab
  • HY-10524
    GSK1904529A
    Inhibitor 99.66%
    GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.
    GSK1904529A
  • 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.
    PQ401
  • HY-10252
    NVP-ADW742
    Inhibitor 99.54%
    NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
    NVP-ADW742
  • HY-N0908
    Ginsenoside Rg5
    Agonist 99.86%
    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
  • HY-15749
    XL228
    Inhibitor 99.29%
    XL228 is a multi-targeted tyrosine kinase inhibitor with IC50s of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.
    XL228
  • HY-13203
    NVP-TAE 226
    Inhibitor 99.92%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity