Cat. No.: HY-19912

Fruquintinib

(Synonyms: HMPL-013)

10 Cited Publications

Customer Review

Based on 10 publication(s) in Google Scholar

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.

Purity: 99.98%
CAS No.: 1194506-26-7
Formula: C₂₁H₁₉N₃O₅
Molecular Weight:393.39

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Fruquintinib Chemical Structure

CAS No.: 1194506-26-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (10)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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)

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 205	IC₅₀	>10 μM Compound: Fruquintinib	Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
HCT-116	IC₅₀	0.8 μM Compound: Fruquintinib	Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
HT-29	IC₅₀	1.5 μM Compound: Fruquintinib	Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
LoVo	IC₅₀	>10 μM Compound: Fruquintinib	Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1194506-26-7
Appearance Solid
Molecular Weight 393.39
Formula C₂₁H₁₉N₃O₅
Color White to off-white
SMILES

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

HMPL-013
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (10)

All Histological Imaging/StainingIn Vivo Efficacy StudyCell Imaging/Staining

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Journal Impact Factor

Cell Death Differ

Exploring fructose metabolism as a potential therapeutic approach for pancreatic cancer. [Abstract]

2024 Dec;31(12):1625-1635. PMID: 39406919

Fruquintinib purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Dec;31(12):1625-1635. [Abstract]

The angiogenesis inhibitor Fruquintinib (Fq) (2 mg/kg; i.g.; once daily) effectively inhibited the expression of CD31 and enhanced the inhibition of 2,5-AM on CD31 in HPAC and MIA Paca2 cell xenograft tumor tissues.

Fruquintinib purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Dec;31(12):1625-1635. [Abstract]

The angiogenesis inhibitor Fruquintinib (Fq) (2 mg/kg; i.g.; once daily) treatment effectively attenuated fructose-induced development of MIA Paca2 cell xenograft tumor.
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Eur J Med Chem

Design, synthesis, and biological evaluation of 1,6-naphthyridine-2-one derivatives as novel FGFR4 inhibitors for the treatment of colorectal cancer. [Abstract]

2023 Nov 5:259:115703. PMID: 37556948

Fruquintinib purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2023 Nov 5:259:115703. [Abstract]

Representative photographs of tumors and quantification in each group from the HCT116 xenograft model after Fruquintinib (10 mg/kg; p.o) or vehicle treatment.

Fruquintinib purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2023 Nov 5:259:115703. [Abstract]

Representative images and quantification of Ki67, CD68, FAK and E-cad. Fruquintinib (10 mg/kg; p.o) suppressed the proliferation (Ki67 stain) and migration (CD68, FAK, E-cad stain) of tumor cells from the HCT116 xenograft model.
Cell Reprogram

Effects of Fruquintinib on the Pluripotency Maintenance and Differentiation Potential of Mouse Embryonic Stem Cells. [Abstract]

2021 Jun;23(3):180-190. PMID: 34077681
J Chromatogr B Analyt Technol Biomed Life Sci

Simultaneous determination of 11 oral targeted antineoplastic drugs and 2 active metabolites by LC-MS/MS in human plasma and its application to therapeutic drug monitoring in cancer patients. [Abstract]

2024 Apr 15:1237:124100. PMID: 38547701
Biochem Biophys Res Commun

DC101, an anti-VEGFR2 agent, promotes high-endothelial venule formation and immune infiltration versus SAR131675 and fruquintinib. [Abstract]

2023 Jun 18:661:10-20. PMID: 37084488

Fruquintinib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2023 Jun 18:661:10-20. [Abstract]

Fruquintinib (2.5 mg/kg; i.g.; once daily for 2 weeks) treatment resulted in slower growth and reduced volume of B16.F1-OVA tumors in C57BL/6 mice.
Growth Factors

Platelet-rich plasma promotes wound repair in diabetic foot ulcer mice via the VEGFA/VEGFR2/ERK pathway. [Abstract]

2024 Oct;42(4):161-170. PMID: 39543829
Chemotherapy

Evaluation of a novel combination therapy, based on trifluridine/tipiracil and fruquintinib, against colorectal cancer. [Abstract]

2023;68(2):102-110. PMID: 36623495
Res Sq

2025 Dec 24.
bioRxiv

Low-Cost Robotic Manipulation of Live Microtissues for Cancer Drug Testing. [Abstract]

2024 Aug 6:2024.03.21.586169. PMID: 38586030

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (12.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.33 mg/mL (0.84 mM); Clear solution

This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.33 mg/mL (0.84 mM); Clear solution

This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 0.33 mg/mL (0.84 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 0.33 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Sun Q, et al. Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5420 mL	12.7100 mL	25.4201 mL	63.5502 mL
	5 mM	0.5084 mL	2.5420 mL	5.0840 mL	12.7100 mL
	10 mM	0.2542 mL	1.2710 mL	2.5420 mL	6.3550 mL

Keywords

Fruquintinib

10 Cited Publications

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Fruquintinib

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FDA Kinase Inhibitor Library

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Publications Citing Use of MedChemExpress (MCE) Fruquintinib

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (10)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Fruquintinib Related Classifications

HY-19912 Related Classifications