| 应用 |
Linsitinib is a selective inhibitor of IGF-1R with IC50 of 35 nM, and modestly potent to InsR with IC50 of 75 nM, and has no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. |
| 产品介绍 |
Linsitinib is a potent, selective insulin-like growth factor-1 receptor (IGF-1R, IC50 = 35 nM) and insulin receptor (IR, IC50 = 75 nM) kinase inhibitor which works to block the autophosphorylation of IGF-1R and IR. Additionally, in vitro studies of Linsitinib have demonstrated its ability to inhibit the proliferation of multiple tumor cell lines. |
| 备注 |
OSI-906 (Linsitinib) is a selective inhibitor of IGF-1R with IC50 of 35 nM; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3. |
| 生化机理 |
Linsitinib is highly potent, orally efficacious and highly selective, dual ATP-competitive tyrosine kinase inhibitor of insulin-like growth factor-1 receptor (IGF-1R) (IC50: 35 nM) and insulin receptor (IR) (IC50: 75 nM). |
| 别名 |
顺式-3-[8-氨基-1-(2-苯基-7-喹啉基)咪唑并[1,5-A]吡嗪-3-基]-1-甲基环丁醇;OSI 906; OSI906; (1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol |
