Sulfatinib (HMPL-012)

A multi-kinase inhibitor

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数量
1mg

￥975.00

780.00

- +
5mg

￥2037.00

1630.00

- +
10mg

￥3125.00

2500.00

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50mg

￥9525.00

7620.00

- +
100mg

￥14825.00

11860.00

- +

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Background

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)

Protocol

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].

参考文献:

[1]. PCT Int. Appl. (2011), WO 2011060746 A1 20110526.