JI-101 - Ephrin Receptor 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEJI-101Cat. No.: HY-16265CAS No.: 900573-88-8分式: CHBrNO分量: 466.33作靶点: Ephrin Receptor; PDGFR; VEGFR作通路: Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (

2、214.44 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1444 mL 10.7220 mL 21.4440 mL5 mM 0.4289 mL 2.1444 mL 4.2888 mL10 mM 0.2144 mL 1.0722 mL 2.1444 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结

3、果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.36 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.36 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% co

4、rn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.36 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 JI-101有服活性的有抗癌活性的多靶点激酶抑制剂，可抑制 VEGFR2，PDGFR 和 EphB4。IC50 & Target VEGFR2 PDGFR体外研究 JI-101 is found to be stable in all preclinical and human liver microsomes. The % metabolized

5、 is rangedbetween 3.03-3.95 across the tested species liver microsomes. The % metabolized is relatively higher inmice liver microsomes followed by dog, human and rat liver microsomes 1.体内研究 JI-101excreted through bile along with its mono- and di-hydroxy metabolites. Following oral administration,JI-

6、101 is rapidly absorbed, reaching Cmax within 2h. The t1/2 of JI-101 with intravenous and oral route isfound to be 1.750.79 and 2.660.13h, respectively. The Cl and Vd by intravenous route for JI-101 are foundto be 13.02.62mL/min/kg and 2.111.42L/kg, respectively. The tissue distribution of JI-101 is

7、 extensivewith rapid and preferred uptake into lung tissue. Overall, the oral bioavailability of JI-101 is 55% and theprimary route of elimination for JI-101 is feces 1.PROTOCOLAnimal Rats: Pharmacokinetics and bioavailability assessment of JI-101 are evaluated in a preliminary parallel-groupAdminis

8、tration 1 study in male S.D. rats. Four rats (195210 g) per route receive JI-101 at a dose of 3 and 30 mg/kg for i. v.(via tail vein) and oral dose (by gavage), respectively. Serial blood samples (100 L) are collected from retro-orbital plexus at pre-dose, 0.12 ( i. v. only) 0.25, 0.5, 1, 2, 4, 8, 1

9、0 (oral only) and 24 h. Blood samples arecollected in tubes containing K2 EDTA as the anticoagulant and centrifuged for 5 min maintained at 4 C forplasma separation and stored frozen at 8010 C until analysis 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Gurav SD, et al. Pharmacokinetics, tissue distribution and identification of putative metabolites of JI-101 - a novel triple kinase inhibitor inrats. Arzneimittelforschung. 2012 Jan;62(1):27-34.McePdfHeightCaution: Product has not been fully validate