产品描述:
The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) promotes cell growth while inhibiting apoptotic pathways. Overexpression of IGF-1R is found in certain solid tumors and hematologic neoplasias.{31137,31135} However, insulin receptor (InsR) signaling can compensate for IGF-1R inhibition.{31134} Linsitinib is a dual inhibitor of IGF-1R and InsR kinases (IC50s = 35 and 75 nM, respectively).{31136} It also inhibits InsR-related receptor (IC50 = 75 nM) but is without effect (IC50 > 10 µM) against a large panel of other kinases.{31136} Linsitinib inhibits proliferation of a variety of tumor cell lines in vitro and has antitumor efficacy in an IGF-1R-driven xenograft mouse model when administered orally.{31136} A rapid, non-invasive method to predict the pharmacodynamic response to linsitinib has been reported.{31134}