现货,NVP-AEW541 ,CAS号:475489-16-8,美国进口,受体酪氨酸激酶(RTK) , IGF-1R, IGF-1R 抑制剂和化合物

信号转导通路: 受体酪氨酸激酶(RTK) >> IGF-1R >> IGF-1R 抑制剂和化合物 >> NVP-AEW541http://selleck.cn/nvp-aew541-S1034.html

技术数据:

分子量(MW): 439.55

化学式:

C27H29N5O

 

溶解度: DMSO ≥88mg/mL Water <1mg/mL Ethanol ≥88mg/mL

纯度: 99%

稳定性: at -20℃ 2 years

CAS号: 475489-16-8

生物活性

 

 

NVP-AEW541 is an IGF-IR inhibitor with an IC50 of median 3.6 μM.

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. [1][2]

 

 

 

参考文献

Down-Regulation of Insulin-Like Growth Factor I Receptor Activity by NVP-AEW541 Has an Antitumor Effect on Neuroblastoma Cells In vivo and In vitro Camillo Mancini, Roberta Vitali, et al. Clin Cancer Res 2006;12:6772-6780

Antitumor Activity of the Insulin-Like Growth Factor-I Receptor Kinase Inhibitor NVP-AEW541 in Musculoskeletal Tumors Maria Cristina Manara, Giordano Nicoletti, et al. Cancer Res 2005;65:3868-3876

 

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