475489-16-8

溶解度:Soluble in DMSO

储存条件:at -20℃ 2 years

生物活性

NVP-AEW541 is a pyrrolo[2,3-d]pyrimidine derivative highly selective against IGF-IR, compared with the insulin receptor and other tyrosine kinases. ^[1]
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. ^[1]
NVP-AEW541 inhibits IGF-I-mediated receptor activation and downstream signaling. In addition to growth inhibition, the drug also induced apoptosis in vitro. Oral ad ministration of NVP-AEW541 (50 mg/kg twice daily) inhibited tumor growth of neuroblastoma xenografts in nude mice. ^[1]
Therapeutic potential of NVP-AEW541 was also analyzed in Ewing’s sarcoma, osteosarcoma, rhabdomyosarcoma, and pancreatic cancer.

参考文献

[1] Barbara Tanno et al. Clin Cancer Res.2006 November 15;12:6772-6780