2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
JI-101 is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 (EphB4). JI-101 inhibits angiogenesis, and subsequently tumor growth.
In vitro :Caco-2 human intestinal epithelial cells were plated in 24-Transwell dual chamber plates (cell density of 500 000 cells/cm2 on day-1). The permeability studies were conducted with the monolayers cultured for 20-23 days in culture. The integrity of each Caco-2 cell monolayer was certified by trans-epithelial electrical resistance (TEER) test (pre-experiment) and by determining the permeability of reference compounds3H-propranolol (high permeability) and 3H-mannitol (low permeability). In addition, the reference substrate 3H-vinblastine was included as a positive control P-gp substrate. The concentration of JI-101 used in the assay was 10 and 100 uM. All the stocks were made in DMSO and the final concentration of DMSO in spiking solution was 0.5%.
in vivo: For oral administration JI-101 was formulated as a suspension with 20 μL of Tween-80 and 0.5% methyl cellulose. Pharmacokinetics and bioavailability assessment of JI-101 were evaluated in a preliminary parallel-group study in male S.D. rats. Four rats (195-210 g) per route received JI-101 at a dose of 3 and 30 mg/kg for i.v. (via tail vein) and oral dose (by gavage), respectively
