1. Protein Tyrosine Kinase/RTK
  2. VEGFR

Fruquintinib (Synonyms: HMPL-013)

Cat. No.: HY-19912 Purity: 99.93%
Handling Instructions

Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively.

For research use only. We do not sell to patients.

Fruquintinib Chemical Structure

Fruquintinib Chemical Structure

CAS No. : 1194506-26-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 132 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 900 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

View All VEGFR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively.

IC50 & Target[1]

VEGFR1

33 nM (IC50)

VEGFR2

35 nM (IC50)

VEGFR3

0.5 nM (IC50)

In Vitro

Fruquintinib demonstrates potent inhibition on VEGF-A dependent KDR phosphorylation in HEK293-KDR cells and VEGF-A induced proliferation in primary HUVECs with IC50s of 0.6±0.2 nM and 1.7 nM, respectively. Similarly, potent VEGFR3 attenuation by fruquintinib is observed in primary HLECs, with IC50s of 1.5 nM and 4.2 nM for VEGF-C stimulated VEGFR3 phosphorylation and proliferation, respectively. Fruquintinib suppresses the tube branching, tube length and area in a concentration-dependent manner. The tubule length of primary HUVECs decreased by 74% and 94% at 0.03 and 0.3 μM of fruquintinib, respectively. Fruquintinib inhibits HUVEC tubule growth and CAM angiogenesis. Tube formation is suppressed significantly after treatment with fruquintinib at 0.3 μM for 18 hours[1].

In Vivo

Gastric cancer BGC-823 model is found to be most sensitive to fruquintinib. In this model, fruquintinib inhibits tumor growth by 62.3% and 95.4∼98.6%, at 0.5 and 2 mg/kg once daily dosing, respectively. When the dose is elevated to 5 mg/kg and 20 mg/kg, the tumors regress by 24.1% and 48.6%, respectively. The level of anti-tumor growth activity of fruquintinib varies in different tumor xenograft models. Fruquintinib significantly decreases the micro-vessel density even at the lowest dose of 0.8 mg/kg[1].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.5420 mL 12.7100 mL 25.4201 mL
5 mM 0.5084 mL 2.5420 mL 5.0840 mL
10 mM 0.2542 mL 1.2710 mL 2.5420 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

Fruquintinib is prepared initially as a 10 mM stock solution in DMSO and diluted in appropriate assay media[1].

Primary HUVECs or HLECs in exponential phase are suspended in 100 μL of RPMI-1640 media containing 0.5% FBS, and seeded at 5000 cell/well in 96-well plates pre-coated with 0.2% gelatin or fibronectin, and incubated overnight in a 5% CO2, 37°C incubator. Fruquintinib and VEGF-A165 or VEGF-C (50 ng/mL) are added and incubated for 48 hours. Viability of the cells is determined using CCK-8 assay format[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Fruquintinib is suspended in aqueous 0.5% CMC-Na (w/v) and stored at 4°C[1].

Mice: The patient derived xenograft models are established after the primary tumor adopted serial passages in vivo. Once tumors have grown to 100-300 mm3, the animals are randomly assigned with 6-8 animals per group. The mice are treated orally with the vehicle (control group) or fruquintinib at a dose range of 0.5-20 mg/kg suspended in the vehicle (treated group) once daily for 3 weeks. In combination studies, docetaxel (Taxotere, 5 mg/kg) or oxaliplatin (10 mg/kg) is administered to nude mouse via intravenous injection, once a week. Tumor size and body weights are measured 3 times a week. Tumor volumes (TV) are calculated[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

393.39

Formula

C₂₁H₁₉N₃O₅

CAS No.

1194506-26-7

SMILES

O=C(C1=C(C)OC2=CC(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)=CC=C12)NC

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 7.75 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.93%

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Inquiry Information

Product Name:
Fruquintinib
Cat. No.:
HY-19912
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