化学名称 : 7-[反式-3-(1-氮杂环丁烷甲基)环丁基]-5-[3-(苯甲氧基)苯基]-7H-吡咯[2,3-D]嘧啶-4-胺
CAS : 475489-16-8
英文名称: NVP-AEW541/AEW541
英文同义词: NVP-AEW541
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