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Description: JI-101 is an orally bioactive multi-kinase inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRb), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities. JI-101 has shown potent in vitro and in vivo anticancer activity against a variety of cancer cell lines and xenografts. It is currently entering Phase II clinical development for the treatment of solid tumors. JI-101 is found to be stable in all preclinical and human liver microsomes. The % metabolized is ranged between 3.03-3.95 across the tested species liver microsomes.The % metabolized is relatively higher in mice liver microsomes followed by dog, human and rat liver microsomes.
References: Arzneimittelforschung. 2012 Jan; 62(1):27-34
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