IGF-1R Inhibitor

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.

JB-1, an IGF-I analog, is a selective IGF-I receptor inhibitor that does not interact with IGF-II. JB-1 competes with IGF-I for binding to IGF-1R and blocks receptor autophosphorylation. JB-1 increases the level of sVEGFR-1. JB-1 normalizes retinal abnormalities, including reducing retinal neovascularization. JB-1 is applicable to studies related to oxygen-induced retinopathy.

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.

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 (K_is=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects.

AZ7550 Mesylate is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.

AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.

Robatumumab (Sch 717454) is an anti-human IGF-1R (insulin-like growth factor receptor-1) antibody. Robatumumab shows anti-tumor activity and anti-proliferative activity to cancer cells. Robatumumab can be used in osteosarcoma and Ewing sarcoma research.

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.

AG 538 is a potent, competitive inhibitor of IGF-1 receptor kinase, with an IC₅₀ of 400 nM.

Indirubin Derivative E804 is a potent inhibitor of Insulin-like Growth Factor 1 Receptor (IGF1R), with an IC₅₀ of 0.65 μM for IGF1R.

Lonigutamab (hz208F2-4) is a humanized anti-IGF-1R monoclonal antibody, serveing as a targeting vector for antibody-drug conjugates (ADCs). Lonigutamab causes G2-M phase cell cycle arrest and increases apoptosis in IGF-1R-overexpressing tumor cells. Lonigutamab demonstrates potent antitumor efficacy in IGF-1R-overexpressing xenograft models. Lonigutamab can be used for the study of Solid tumors with overexpression of IGF-1R and thyroid eye diseases.

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.

IGF-1R inhibitor-2 (example 121) is an insulin-like growth factor-1 receptor (IGF-1R) inhibitor. Downregulation of IGF-1R can reverse the transformed phenotype of tumor cells and potentially render them susceptible to apoptosis.

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.

IGF-1R/SRC-IN-1 (Compound 3b) is an inhibitor for IGF-1R (IC₅₀ is 63 μM) and SRC.

Elegrobart is an immunoglobulin G1-κ monoclonal antibody targeting the human insulin-like growth factor 1 receptor (IGF1R). Elegrobart is promising for research of diseases associated with abnormal IGF1R signaling, especially thyroid eye disease.

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.

Ceritinib (LDK378)-d₇ is a deuterium labeled Ceritinib (HY-15656). Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor. 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.

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).

AZ7550 hydrochloride is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.