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-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-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-100038
    AZD9362
    Inhibitor
    AZD9362 is a reversible, ATP-competitive and orally active small molecule inhibitor of IGF-1R and insulin receptor. AZD9362 inhibits the IGF-1R enzyme with an IC50 of 14 nM. AZD9362 can enhance the anti-tumor effect of AZD5363 (HY-15431). AZD9362 can be used for the research of cancer, such as breast cancer.
    AZD9362
  • 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-182264
    Masoprocol tetrapivalate
    Inhibitor
    Masoprocol tetrapivalate (Nordihydroguaiaretic acid tetrapivalate) is a catecholic butane metabolite and also a tyrosine kinase activity inhibitor of IGF-1R and EGFR. Masoprocol tetrapivalate regulates tyrosine kinase signaling pathways associated with cell proliferation. Masoprocol tetrapivalate can be used in the research of proliferative diseases, including malignant, precancerous or benign cancers, and solid tumors.
    Masoprocol tetrapivalate
  • HY-10252A
    cis-NVP-ADW742
    Inhibitor
    cis-NVP-ADW742 (cis-ADW742) is a cis isomer of NVP-ADW742 (HY-10252). NVP-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.
    cis-NVP-ADW742
  • 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-P991253
    BIIB022
    Inhibitor
    BIIB022 is a human IgG4 monoclonal antibody (mAb) targeting IGF1R/CD221. BIIB022 blocks IGF-1 and IGF-2-induced phosphorylation of IGF-1R and downstream substrates. BIIB022 can be used in lung, pancreatic, and colon cancer research. Recommended isotype control: Human IgG4 kappa, Isotype Control (HY-P99003).
    BIIB022
  • HY-P991255
    VRDN-002
    Inhibitor
    VRDN-002 is a human monoclonal antibody (mAb) targeting IGF1R/CD221. VRDN-002 reduces inflammation and proptosis in thyroid eye disease (TED). VPI-2690B can be used in Graves ophthalmopathy research.
    VRDN-002
  • HY-10200R
    BMS-754807 (Standard)
    Inhibitor
    BMS-754807 (Standard) is the analytical standard of BMS-754807 (HY-10200). This product is intended for research and analytical applications. 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 (Standard)
  • HY-41404R
    Piperonylic acid (Standard)
    Piperonylic acid (Standard) is the analytical standard of Piperonylic acid. This product is intended for research and analytical applications. Piperonylic acid is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic Acid is a selective, mechanism-based inactivator of the trans-cinnamate 4-Hydroxylase. Piperonylic acid has anticancer, antioxidant and antibacterial activities.
    Piperonylic acid (Standard)
  • HY-P990966
    Redalsomatropin alfa
    Redalsomatropin alfa (JR-142) is a recombinant long-acting growth hormone. Redalsomatropin alfa extends its half-life through fusion with modified serum albumin. Redalsomatropin alfa is well-tolerated and can maintain IGF-1 levels. Redalsomatropin alfa can be used in research related to growth hormone deficiency.
    Redalsomatropin alfa
  • 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
    Ceritinib (Standard) is the analytical standard of Ceritinib (HY-15656). This product is intended for research and analytical applications. Ceritinib is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib 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-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)
  • HY-14357
    BMS 695735
    Inhibitor
    BMS 695735 (compound 10) is an inhibitor of IGF-1R with an IC50 value of 0.034 μM. BMS 695735 has anti-tumor activity.
    BMS 695735
  • HY-10524R
    GSK1904529A (Standard)
    Inhibitor
    GSK1904529A (Standard) is the analytical standard of GSK1904529A (HY-10524). This product is intended for research and analytical applications. 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 (Standard)
  • HY-10262R
    BMS-536924 (Standard)
    Inhibitor
    BMS-536924 (Standard) is the analytical standard of BMS-536924 (HY-10262). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity