Fruquintinib (HMPL-013)

Catalog No.S5667

For research use only.

Fruquintinib (HMPL-013) 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.

Fruquintinib (HMPL-013) Chemical Structure

CAS No. 1194506-26-7

Selleck's Fruquintinib (HMPL-013) has been cited by 2 Publications

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Biological Activity

Description Fruquintinib (HMPL-013) 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 Research:

[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 Research:

[1]

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 393.39
Formula

C21H19N3O5

CAS No. 1194506-26-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C2=C(O1)C=C(C=C2)OC3=NC=NC4=CC(=C(C=C43)OC)OC)C(=O)NC

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04577963 Recruiting Drug: Fruquintinib|Drug: Tislelizumab Triple Negative Breast Cancer|Endometrial Cancer|Solid Tumor Unspecified Adult|Colorectal Cancer Hutchison Medipharma Limited|BeiGene August 9 2021 Phase 1|Phase 2
NCT04716634 Recruiting Drug: Tislelizumab|Drug: Fruquintinib Advanced Solid Tumors BeiGene|Hutchison Medipharma Limited April 19 2021 Phase 2
NCT04557397 Completed Drug: Fruquintinib|Drug: Itraconazole|Drug: Rifampin Drug Drug Interaction Hutchison Medipharma Limited|Covance September 2 2020 Phase 1
NCT02689752 Completed Drug: fruquintinib Healthy Hutchison Medipharma Limited July 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

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