| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 1mg | ¥406.00 | 现货 | 1 | |
| 5mg | ¥945.00 | 现货 | 1 | |
| 10mg | ¥1,470.00 | 现货 | 1 | |
| 25mg | ¥2,564.00 | 现货 | 1 | |
| 50mg | ¥3,710.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥999.00 | 现货 | 1 |
Sulfatinib is a multi-kinase inhibitor.1 It inhibits the receptor tyrosine kinases VEGFR1, VEGFR2, VEGFR3, FGFR1, colony stimulating factor 1 receptor (CSF1R), tropomyosin-related kinase B (TrkB), and FMS-related tyrosine kinase 3 (FLT3; IC50s = 2, 24, 1, 15, 4, 41, and 67 nM, respectively). It is selective for these kinases over a panel of 278 kinases (IC50s = >150 nM for all).
1.Qi, C., and Xu, J.Method of treating solid tumorsWO2018090324A1(2018)
Kinase experiment: | The KDR kinase inhibition activity is tested using the the Z-lyte assay kit. The testing system contains 300 ng/mL of recombinant human KDR catalytic domain, 10 μM of ATP, 1 μM of substrate peptide, and a test compound (Sulfatinib) at a series of different concentrations in 384-well plate; total volume is 10 μL. The enzyme inhibition proceeds at room temperature (25°C), for 1 hour at room temperature on the shaker. 5 μL of stop solution is added to stop the reaction[2]. |
Animal experiment: | The phamacokinetics of Sulfatinib are studied with male ICR mice (n=6 for each group, weight 20-30g) after a single intraveneous and oral dosing at 2.5 and 10mg/kg, respectively. For i.v. dosing formulation, Sulfatinib is dissolved in DMSO (0.25%)-solutol(10%)-ethanol(10%)-physiological saline(79.75%) at the concentration of 0.25 mg/mL. And the p.o. Dosing formulation (1mg/mL) is prepared with 0.5% CMC-Na. After i.v. Or p.o. Dosing, blood samples are collected via the ophthalmic vein at 0 (pre-close), 5, 15, 30 min and 1, 1.5, 2, 4, 8, 24 h, anti-coagulated with heparin-Na. After centrifugation, plasma samples are seprated and protein precipitated with acetonitrilel containing internal standard[2]. |
References: [1]. PCT Int. Appl. (2011), WO 2011060746 A1 20110526. |
