IGF-1R

OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

AZ7550 trimesylate salt (AZ7550 Mesylate) is the active metabolite of ositinib, AZ7550 trimesylate salt inhibits IGF1R activity and can be used in the study of non-small cell lung cancer.

IGF-1Rinhibitor-4 (compound 22) is a potent inhibitor of IGF-1R, demonstrating an inhibition rate of 63% at a concentration of 10 μM. This compound plays a significant role in cancer research.

IGF-1Rinhibitor-5 (compound 19) is a potent IGF-1R inhibitor with an IC50 of 6 μM, showing potential for cancer research.

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19 42 14 150 nM, for MLK1 MLK2 MLK3 DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

NVP-ADW742 (ADW) is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.

Teprotumumab is a human monoclonal antibody that blocks the IGF-1 receptor (IGF-1R). Teprotumumab binds to the extracellular α-subunit domain ligand of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab reduces TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used in the study of thyroid-associated eye diseases.

Xentuzumab (BI836845) is a recombinant monoclonal antibody to humanised IGF ligand that inhibits IGF1 and IGF2 growth-promoting signalling and inhibits AKT activation for the study of solid tumours.

Ganitumab (AMG 479) is a highly potent monoclonal antibody targeting the type 1 insulin-like growth factor receptor (IGF1R). Recognized for binding IGF1R at low concentrations with a KD value of 0.22 nM, Ganitumab inhibits IGF1R interactions with IGF1 and IGF2 in mice, making it useful for cancer research.

Lonigutamab (hz208F2-4) is a humanized monoclonal antibody targeting the insulin-like growth factor-1 receptor (IGF-1R) for the study of thyroid eye disease.

Cixutumumab (IMC-A12) is a humanized IgG monoclonal antibody targeting the insulin-like growth factor 1 receptor (IGF1R). It has anticancer activity, inhibits ligand-dependent receptor activation and downstream signaling, and can be used in the study of non-small cell lung and prostate cancer.

Tyrphostin AG 538 is a chalcone compound, an IGF-1 receptor kinase inhibitor (IC₅0 : for 400 nM) that is potent, cell-permeable, reversible, and competitive.

WAY-270250 is an IGF-1R SRC inhibitor.

NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.

Protonstatin-1 is used as a hypoglycemic agent and as a compound for the treatment of Alzheimer's disease, inhibits IGFIR kinase activity and can be used in cancer research.

IGF-1R inhibitor-2 (example 121) is a compound that inhibits the insulin-like growth factor-1 receptor (IGF-1R), potentially reversing the transformed phenotype of tumor cells and increasing their susceptibility to apoptosis.

IGF-1R Inhibitor-3 (Compound C11) serves as an allosteric inhibitor targeting the kinase of insulin-like growth factor receptor 1 (IGF-1R), exhibiting an IC50 value of 0.2 μM [1].

IGF-1Rmodulator 1 (Example 5) is an IGF-1R modulator featuring an EC50 of 0.29 μM (FGFR1), 0.25 μM (IGF1R), 0.34 μM (TrkA), and 0.39 μM (TrkB). This compound is useful in research on diseases characterized by impaired signaling of neurotrophic and or other trophic factors, such as Alzheimer's disease.

Insulin (human) is a peptide hormone that promotes glycogen synthesis and regulates glucose levels in the blood. Insulin (human) has hypoglycemic activity and is used clinically to treat hyperglycemia in diabetic patients.

GIP (3-42), human (Gastric Inhibitory Polypeptide (3-42) (human)) is a peptide that acts as a glucose-dependent proinsulinotropic polypeptide (GIP) receptor antagonist and regulates insulin secretion and the metabolic effects of GIP in vivo, which can be used to study type 2 diabetes.

Urolithin C is a gut metabolite of ellagic acid. Urolithin C induces apoptosis in PC12 cells through a mitochondria-mediated pathway.

Robatumumab (Sch 717454) is a fully human anti-insulin-like growth factor receptor type 1 (IGF-1R) monoclonal antibody with antitumor and antiproliferative activity.Robatumumab is used in the study of ovarian cancer.

Insulin efsitora alfa (LY-3209590) is a selective insulin receptor (IR) agonist and fusion protein that combines a novel single-chain insulin variant with the structural domain of human IgG Fc for the study of type 2 diabetes.

Dusigitumab (MEDI 573) is a human IgG2λ monoclonal antibody targeting insulin-like growth factors IGF2 and IGF1, offering therapeutic potential for conditions related to these proteins [1].