NVP-ADW742

NVP-ADW742是一种新的IFG-1受体(IGF-1R)激酶抑制剂,IC50值为0.17 μM[1].

NVP-ADW742对IGF-1R比对胰岛素受体(InsR)更有效(超过16倍).此外,NVP-ADW742也可抑制其他激酶,对HER2\PDGFR\VEGFR-2或Bcr-Abl p210的IC50值大于10 μM,对c-Kit的IC50值大于5 μM[1].另外,在针对包括H526\H146\WBA和H209细胞系的小细胞肺癌(SCLC)的MTT试验中,NVP-ADW742与依托泊苷和卡铂联合使用可抑制细胞生长,诱发细胞毒性.除此之外,NVP-ADW742可完全抑制H526细胞中IGF-I诱导的VEGF mRNA表达[2].

参考文献：
[1] Mitsiades CS1, Mitsiades NS, McMullan CJ, Poulaki V, Shringarpure R, Akiyama M, Hideshima T, Chauhan D, Joseph M, Libermann TA, García-Echeverría C, Pearson MA, Hofmann F, Anderson KC, Kung AL.  Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors . Cancer Cell. 2004 Mar; 5(3):221-30.
[2]Warshamana-Greene GS1, Litz J, Buchdunger E, García-Echeverría C, Hofmann F, Krystal GW.  The insulin-like growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy. Clin Cancer Res. 2005 Feb 15;11(4):1563-71.