Foretinib

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Foretinib

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	849217-64-7
包装:	2mg, 5mg, 10mg, 50mg, 100mg

包装与价格：

产品名称

XL880, GSK1363089

产品介绍

Foretinib (GSK1363089)是一种ATP竞争性的HGFR和VEGFR抑制剂，作用于Met和KDR作用最强，IC50分别为0.4 nM和0.9 nM，对Ron， Flt-1/3/4， Kit， PDGFRα/β和Tie-2作用效果稍弱，对FGFR1和EGFR几乎没有抑制活性。

细胞实验
细胞系	B16F10 cells
方法	HGF-induced migration assay. B16F10 cells (2 *105) were seeded onto 0.8 Am membranes in the top chamber of a 96-well Transwell plate in DMEM containing a serial dilution of EXEL-2880 and 0.1% FBS. DMEM containing HGF (50 ng/mL), 0.2% FBS, and EXEL-2880(foretinib) was added to the bottom chamber, and after 24 h, the medium was removed and Accutase (ISC BioExpress) was added to the bottom chamber. After 30 min, cells were transferred to a V-bottomed 96-well plate, centrifuged, and resuspended in HBSS containing 2 mg/mL calcein-AM (Molecular Probes). After incubation for 30 min, cells were transferred into a black 96-well plate. Fluorescence emission was measured at 480 nm using an excitation wavelength of 520 nm and imaged with a fluorescence microscope.
浓度	14, 41, 123nM
处理时间	24h

动物实验
动物模型	ligand (e.g., HGF or VEGF)–induced receptor phosphorylation of Met in liver and Flk-1/KDR in lung
配制	0.9% saline
剂量	100 mg/kg
给药处理	oral gavage

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.5807 mL	7.9033 mL	15.8065 mL
5 mM	0.3161 mL	1.5807 mL	3.1613 mL
10 mM	0.1581 mL	0.7903 mL	1.5807 mL