Fruquintinib

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Chemical Structure| 1194506-26-7 同义名 : HMPL-013
CAS号 : 1194506-26-7
货号 : A830869
分子式 : C21H19N3O5
纯度 : 99%+
分子量 : 393.393
MDL号 : MFCD28502149
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(22.88 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Fruquintinib (HMPL-013) acts as a potent, selective inhibitor for VEGFR 1/2/3, exhibiting IC50 values of 33 nM, 0.35 nM, and 35 nM, correspondingly[1]. Fruquintinib shows strong inhibitory effects on VEGF-A mediated KDR phosphorylation in HEK293-KDR cells and blocks VEGF-A triggered growth in primary HUVECs, with IC50 values of 0.6±0.2 nM and 1.7 nM, respectively. Fruquintinib also significantly reduces VEGFR3 activity in primary HLECs, evident from IC50s of 1.5 nM and 4.2 nM for VEGF-C induced VEGFR3 phosphorylation and proliferation, respectively. It effectively diminishes tube formation, branching, and expansion in a dose-dependent manner, reducing tubule length in primary HUVECs by 74% and 94% at concentrations of 0.03 μM and 0.3 μM, respectively. Fruquintinib's capability to inhibit tubule development and CAM angiogenesis is noted, with substantial suppression of tube formation after 18 hours at 0.3 μM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.71mL

2.54mL

1.27mL

25.42mL

5.08mL

2.54mL
参考文献

[1]Sun Q, et al. Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.