Size | Price | Stock |
---|---|---|
5mg | $90 | In-stock |
10mg | $160 | In-stock |
50mg | $550 | In-stock |
100mg | $950 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-16265 |
M.Wt: | 466.33 |
Formula: | C22H20BrN5O2 |
Purity: | >98 % |
Solubility: | DMSO : ≥ 100 mg/mL (214.44 mM) |
JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity. IC50 & Target: VEGFR2, PDGFRβ, EphB4[1] 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[1]. 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[1].
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