Fruquintinib

Catalog No.S5667 Batch:S566702

Technical Data

Formula	C₂₁H₁₉N₃O₅
Molecular Weight	393.39	CAS No.	1194506-26-7
Solubility (25°C)*	In vitro	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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

Targets

VEGFR3 ^[1] (Cell-free assay)	VEGFR1 ^[1] (Cell-free assay)	VEGFR2 ^[1] (Cell-free assay)
0.5 nM	33 nM	35 nM

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].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Primary HUVEC cells Concentrations 0.005, 0.05, 0.5 μM Incubation Time 18 hours Method 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.
Animal Study:^{^[1]}	Animal Models Female Balb/c nude mice at the age of 10-11 weeks Dosages 2.5 mg/kg Administration oral

Cell Assay:^{^[1]}

Cell lines
Primary HUVEC cells
Concentrations
0.005, 0.05, 0.5 μM
Incubation Time
18 hours
Method
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.

Animal Study:^{^[1]}

Animal Models
Female Balb/c nude mice at the age of 10-11 weeks
Dosages
2.5 mg/kg
Administration
oral

References

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

Selleck's Fruquintinib has been cited by 3 publications

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

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SHIPPING AND STORAGE
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