IGF-1R 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.

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.

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.

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).

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.

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-554417 is an orally active inhibitor of insulin receptor and insulin-like growth factor-I receptor (IGF-1R) kinases, with IC₅₀ values of 50.6 nM and 67.9 nM, respectively. BMS-554417 blocks downstream signal transduction via the ERK and PI3K/Akt pathways. BMS-554417 induces G0-G1 cell cycle arrest, prevents cyclin D1 accumulation in the nucleus, triggers mitochondrial pathway-mediated apoptosis, promotes HER2 phosphorylation, and inhibits the proliferation and growth of cancer cells. BMS-554417 can be used in research related to colon cancer, ovarian cancer, and breast cancer.

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.

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.

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.

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.

BMS 695735 (compound 10) is an inhibitor of IGF-1R with an IC₅₀ value of 0.034 μM. BMS 695735 has anti-tumor activity.

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.

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.

RKS262 is an orally active cyclin/CDK inhibitor. RKS262 is also an apoptosis inducer and cell cycle regulator, exhibiting cytotoxic activity against cancer cells. RKS262 induces caspase-3 cleavage, ROS generation, SAPK/JNK activation, and upregulates the expression of p53, Bid, Bad, Bok, and p27. RKS262 inhibits the expression of Bcl-2, Mcl-1, Bcl-xL, p21, cyclin D1, cyclin B1, cdc-2, cyclin D4, and DNA-pk KU-80 subunit. RKS262 suppresses the phosphorylation of the IGF-1R/PI3K/PKC pathway, ras oncogene activity, and Cdk-6, while increasing total Akt expression. RKS262 induces G₂/M or S phase cell cycle arrest, disrupts mitochondrial transmembrane potential, and reduces tumor burden in xenograft models. RKS262 is used in research on neuroblastoma and ovarian cancer.

Ceritinib (LDK378) dihydrochloride (Standard) is the analytical standard of Ceritinib dihydrochloride (HY-15656A). This product is intended for research and analytical applications. Ceritinib dihydrochloride is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC₅₀ of 200 pM. Ceritinib dihydrochloride also inhibits IGF-1R, InsR, and STK22D with IC₅₀ values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency.

AG1024 (Standard) is the analytical standard of AG1024 (HY-10253). This product is intended for research and analytical applications. AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC₅₀ of 7 μM. AG1024 inhibits phosphorylation of IR (IC₅₀=57 μM). AG1024 induces apoptosis and has anti-cancer activity.

CL-A3-7 is a virus-cell fusion inhibitor targeting the RSV F protein. It exerts its effect by blocking the interaction between the virus and the host IGF1R, effectively inhibiting infections of both wild-type RSV and the K394R variant. It is applicable to anti-RSV drug development and resistance-related research.

NVP-ADW742 (Standard) is the analytical standard of NVP-ADW742 (HY-10252). This product is intended for research and analytical applications. 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.