Home Angiogenesis VEGFR inhibitor Fruquintinib For research use only.

Fruquintinib

Synonyms: HMPL-013

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.

Fruquintinib Chemical Structure

Fruquintinib Chemical Structure

CAS: 1194506-26-7

Selleck's Fruquintinib has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.96%
99.96

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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 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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Female Balb/c nude mice at the age of 10-11 weeks
Dosages 2.5 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04577963 Recruiting Triple Negative Breast Cancer|Endometrial Cancer|Solid Tumor Unspecified Adult|Colorectal Cancer Hutchison Medipharma Limited|BeiGene|Hutchmed August 9 2021 Phase 1|Phase 2
NCT04716634 Active not recruiting Advanced Solid Tumors BeiGene|Hutchison Medipharma Limited April 19 2021 Phase 2
NCT04557397 Completed Drug Drug Interaction Hutchison Medipharma Limited|Covance|Hutchmed September 2 2020 Phase 1
NCT04322539 Active not recruiting Metastatic Colorectal Cancer|Metastatic Colon Cancer Hutchison Medipharma Limited|Hutchmed August 12 2020 Phase 3

Chemical lnformation & Solubility

Molecular Weight 393.39 Formula

C21H19N3O5
CAS No. 1194506-26-7 SDF --
Smiles CC1=C(C2=C(O1)C=C(C=C2)OC3=NC=NC4=CC(=C(C=C43)OC)OC)C(=O)NC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 6 mg/mL ( (15.25 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL


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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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