Fruquintinib

Catalog No.S5667 Batch:S566702

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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

Selleck's Fruquintinib has been cited by 4 publications

Pericyte signaling via soluble guanylate cyclase shapes the vascular niche and microenvironment of tumors [ EMBO J, 2024, 43(8):1519-1544] PubMed: 38528180
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
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.