Fruquintinib (HMPL-013)

Catalog No.S5667

Fruquintinib (HMPL-013) Chemical Structure

Molecular Weight(MW): 393.39

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.

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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

Cell Research:

[1]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Female Balb/c nude mice at the age of 10-11 weeks
  • Formulation: 0.5% aqueous CMC-Na
  • Dosages: 2.5 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 6 mg/mL (15.25 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 393.39
Formula

C21H19N3O5

CAS No. 1194506-26-7
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID