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CAS No. : 900573-88-8
MCE 国际站:JI-101
产品活性:JI-101是有口服活性的有抗癌活性的多靶点激酶抑制剂,可抑制 VEGFR2,PDGFRβ 和 EphB4。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点: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 Cmax within 2 h. The t1/2 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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