NVP-AEW541 is an IGF-IR inhibitor with an IC50 of median 3.6 ¦ÌM. NVP-AEW541 is a pyrrolo[2,3-d]pyrimidine derivative highly selective against IGF-IR, compared with the insulin receptor and other tyrosine kinases. In a panel of 10 neuroblastoma cell lines positive for IGF-IR expression, NVP-AEW541 inhibited in vitro proliferation in a submicromolar/micromolar (0.4-6.8) range of concentrations. NVP-AEW541 inhibits IGF-I-mediated receptor activation and downstream signaling. In addition to growth inhibition, NVP-AEW541 also induced apoptosis in vitro. Oral administration of NVP-AEW541 (50 mg/kg twice daily) inhibited tumor growth of neuroblastoma xenografts in nude mice. Therapeutic potential of NVP-AEW541 was also analyzed in Ewing¡¯s sarcoma, osteosarcoma, rhabdomyosarcoma, and pancreatic cancer.

June 21, 2017

prudect name : NVP-AEW541 is an IGF-IR inhibitor with an IC50 of median 3.6 ¦ÌM.
NVP-AEW541 is a pyrrolo[2,3-d]pyrimidine derivative highly selective against IGF-IR, compared with the insulin receptor and other tyrosine kinases. In a panel of 10 neuroblastoma cell lines positive for IGF-IR expression, NVP-AEW541 inhibited in vitro proliferation in a submicromolar/micromolar (0.4-6.8) range of concentrations. NVP-AEW541 inhibits IGF-I-mediated receptor activation and downstream signaling. In addition to growth inhibition, NVP-AEW541 also induced apoptosis in vitro. Oral administration of NVP-AEW541 (50 mg/kg twice daily) inhibited tumor growth of neuroblastoma xenografts in nude mice. Therapeutic potential of NVP-AEW541 was also analyzed in Ewing¡¯s sarcoma, osteosarcoma, rhabdomyosarcoma, and pancreatic cancer.
NVP-AEW 541

Synonyms: CAS NO: 475489-16-8Molecular Formula: C₂₇H₂₉N₅OMolecular Weight: 439.55Purity: 98%Solubility: In DMSOStorage: -20°C

web site: www.medchemexpress.com

References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18537197