Fruquintinib

製品コードS5667 バッチS566702

化学情報

	Synonyms	HMPL-013	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₁H₁₉N₃O₅
	分子量	393.39	CAS No.	1194506-26-7
Solubility (25°C)*	体外	DMSO	6 mg/mL (15.25 mM)
		Water	˂1 mg/mL
		Ethanol	˂1 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Fruquintinib is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases.
in vitro	In in vitro enzymatic and cellular assays, Fruquintinib inhibits VEGFR family kinases and suppressed VEGF/VEGFR cell signaling in human umbilical vein endothelial cell (HUVEC) and human lymphatic endothial cell (HLEC) with IC50 at low nanomolar level. Few kinases are inhibited other than VEGFRs in a panel of 253 kinases test. Fruquintinib is a highly potent inhibitor of VEGF-induced angiogenesis^[1].
in vivo	Fruquintinib demonstrates favorable pharmacokinetic profile in multiple animal species, oral administration of fruquintinib strongly suppressed VEGF-induced VEGFR2 phosphorylation in the lung tissue in mice. The extent and duration of the inhibition of VEGFR2 phosphorylation correlated well with drug exposures. The strong anti-angiogenic effect resulted in robust anti-tumor efficacy in a number of human tumor xenograft models with good dose response^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Primary HUVEC cells
	濃度	0.005, 0.05, 0.5 μM
	反応時間	18 hours
	実験の流れ	Primary HUVEC cells at 2 × 10⁴ cells/well were seeded in flat bottomed 96-well plates with 100 mL media containing 0.5% FBS. The next day, cells were treated with fruquintinib for 18 hours at 37 C. The cell survival was determined by AlamarBlue assay. The plates were incubated for 3 hours at 37 C and fluorescence value was read at Ex 530 nm and Em 590 nm on Tecan.
動物実験	動物モデル	Female Balb/c nude mice at the age of 10-11 weeks
	投薬量	2.5 mg/kg
	投与方法	oral

参考

[1] Sun Q, et al. Cancer Biol Ther. 2014, 15(12):1635-45.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Tumor-derived insulin-like growth factor-binding protein-1 contributes to resistance of hepatocellular carcinoma to tyrosine kinase inhibitors [ Cancer Commun (Lond), 2023, 10.1002/cac2.12411]	PubMed: 36825684
PDGF signaling inhibits mitophagy in glioblastoma stem cells through N6-methyladenosine [ Dev Cell, 2022, 57(12):1466-1481.e6]	PubMed: 35659339
PDGF Signaling Promotes Mitophagy in Glioblastoma Stem Cells Through N 6-Methyladenosine [ CellPress, 2021, None]	PubMed: None

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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