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JI-101

CAS No. : 900573-88-8

產品活性：JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.

研究領域：Protein Tyrosine Kinase/RTK

作用靶點：Ephrin Receptor  |  PDGFR  |  VEGFR

In Vitro: 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.

In Vivo: JI-101excreted through bile along with its mono- and di-hydroxy metabolites. Following oral administration, JI-101 is rapidly absorbed, reaching C_max within 2?h. The t_1/2 of JI-101 with intravenous and oral route is found to be 1.75±0.79 and 2.66±0.13?h, respectively. The Cl and Vd by intravenous route for JI-101 are found to be 13.0±2.62?mL/min/kg and 2.11±1.42?L/kg, respectively. The tissue distribution of JI-101 is extensive with rapid and preferred uptake into lung tissue. Overall, the oral bioavailability of JI-101 is 55% and the primary route of elimination for JI-101 is feces.

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