NVP-AEW541

一种IGF-1R抑制剂（无细胞测定中IC50=0.15µM）；在20种激酶中对IGF-1R具有选择性，但也抑制InsR、FLT1、FLT3和Tie2（无细胞测定中IC50s分别为0.14、0.6、0.42和0.53µM）；在细胞中选择性抑制IGF-1R自身磷酸化，而非InsR、EGFR、PDGFR、c-Kit和Bcr-Abl（IC50s分别为0.086、2.3、>10、>10、>5和>10µM）；每天两次以20、30或50mg/kg的剂量给药，可缩小NWT-21鼠纤维肉瘤模型中的肿瘤体积。An IGF-1R inhibitor (IC50 = 0.15 µM in a cell-free assay); selective for IGF-1R over a panel of 20 kinases but also inhibits InsR, FLT1, FLT3, and Tie2 (IC50s = 0.14, 0.6, 0.42, and 0.53 µM, respectively, in cell-free assays); selectively inhibits the autophosphorylation of IGF-1R over InsR, EGFR, PDGFR, c-Kit, and Bcr-Abl in cells (IC50s = 0.086, 2.3, >10, >10, >5, and >10 µM, respectively); reduces tumor volume in an NWT-21 murine fibrosarcoma model at 20, 30, or 50 mg/kg twice per day.分子式C27H29N5O分子量439.6NC1=C2C(N([C@@H]3C[C@H](CN4CCC4)C3)C=C2C5=CC=CC(OCC6=CC=CC=C6)=C5)=NC=N1