Fruquintinib (HMPL-013)

製品コードS5667 バッチS566703

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	13 mg/mL (33.04 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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は、VEGFR familyに対し強力な効力と高い選択性を持つ低分子阻害剤です。VEGFR 1、2、3をそれぞれ33 nM、35 nM、0.5 nMのIC50値で阻害し、RET、FGFR-1、およびc-kitキナーゼに対しては弱い阻害しか示しません。
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. This compound is a highly potent inhibitor of VEGF-induced angiogenesis.
in vivo	Fruquintinib demonstrates favorable pharmacokinetic profile in multiple animal species, oral administration of this compound 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.

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

https://pubmed.ncbi.nlm.nih.gov/25482937/

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：

Low-cost robotic manipulation of live microtissues for cancer drug testing [ Sci Adv, 2025, 11(20):eads1631]	PubMed: 40367160
Pericyte signaling via soluble guanylate cyclase shapes the vascular niche and microenvironment of tumors [ EMBO J, 2024, 43(8):1519-1544]	PubMed: 38528180
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
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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