Fruquintinib | CAS 1194506-26-7 | Selective VEGFR Inhibitor for Oncology Research

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Fruquintinib | CAS 1194506-26-7 | Selective VEGFR Inhibitor for Oncology Research

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Fruquintinib (CAS 1194506-26-7) is a potent, orally bioavailable selective small-molecule inhibitor of VEGFR-1, VEGFR-2, and VEGFR-3. It is extensively used in preclinical oncology research to study tumor angiogenesis inhibition, vascular remodeling, tumor proliferation suppression, and VEGFR-mediated signaling pathways.

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Description

Product Description

Fruquintinib is a synthetically designed, highly selective inhibitor of vascular endothelial growth factor receptors (VEGFR1, VEGFR2, VEGFR3), developed to explore anti-angiogenic mechanisms and tumor growth control in preclinical oncology research. The compound’s molecular architecture features heteroaryl and fluorinated groups that confer metabolic stability, high receptor affinity, and enhanced bioavailability in experimental models.

In vitro studies demonstrate that Fruquintinib effectively inhibits endothelial cell proliferation, migration, and tube formation by selectively blocking VEGFR-mediated signaling. By suppressing VEGFR1–3 phosphorylation, Fruquintinib prevents activation of downstream MAPK, PI3K/AKT, and ERK pathways, crucial for angiogenesis and tumor vascular remodeling.

Preclinical models have shown that Fruquintinib reduces microvessel density, disrupts neovascularization, and limits nutrient supply to tumor tissues. Researchers use Fruquintinib to study vascular normalization, tumor perfusion, and combination therapy effects in xenografts and 3D culture systems.

Fruquintinib is highly soluble in DMSO and ethanol, slightly soluble in water, and demonstrates excellent stability under laboratory storage conditions. Its purity (≥99%) ensures reproducible results across in vitro and in vivo experiments.

Experimental applications include:

  • Angiogenesis inhibition studies: Endothelial tube formation, sprouting assays, and microvessel quantification.

  • Tumor proliferation analysis: Investigating VEGFR-driven tumor growth, cell cycle progression, and apoptosis.

  • Tumor microenvironment research: Examining endothelial-tumor interactions and vessel normalization processes.

  • Combination therapy assessment: Evaluating synergistic effects with chemotherapeutic, targeted, or immunotherapeutic agents.

  • Resistance mechanism studies: Understanding compensatory angiogenic signaling under chronic VEGFR blockade.

Fruquintinib’s unique profile as a selective VEGFR inhibitor makes it a valuable tool for mechanistic oncology research and preclinical tumor growth studies.


Product Specifications

ItemDetails
Product NameFruquintinib
CAS Number1194506-26-7
SynonymsHMPL-013; Fruquintinib mesylate; VEGFR inhibitor Fruquintinib
Molecular FormulaC22H16F3N5O2
Molecular Weight437.40 g/mol
Purity≥99%
AppearanceWhite to off-white crystalline powder
SolubilitySoluble in DMSO, ethanol; slightly soluble in water
Storage Temperature2–8 °C, protected from light and moisture
CategorySmall-molecule VEGFR inhibitor
ApplicationsOncology research, angiogenesis inhibition, tumor proliferation studies, tumor microenvironment research
FormulationSuitable for in vitro kinase assays, cell culture studies, and preclinical in vivo models
StabilityStable under recommended laboratory storage conditions
Shelf Life24 months
Supplier TypeResearch chemical supplier
Intended UseFor laboratory research use only
Packaging Options10 mg – 1 kg sealed powder in moisture-proof containers
Delivery ModeCold-chain logistics with tracking and insurance

Mechanism of Action

Fruquintinib selectively binds to VEGFR1, VEGFR2, and VEGFR3 at the ATP-binding site, preventing receptor autophosphorylation and downstream signaling. This blockade suppresses endothelial proliferation, migration, and new vessel formation, which are essential for tumor angiogenesis.

VEGFR Inhibition:
Fruquintinib reduces endothelial proliferation and migration, decreasing tumor vascular density and limiting neovascularization in preclinical models.

Downstream Signaling Suppression:
It inhibits ERK, AKT, and MAPK phosphorylation, inducing cell cycle arrest and apoptosis in tumor cells.

Tumor Microenvironment Modulation:
By disrupting vascular support, Fruquintinib affects nutrient delivery, hypoxia regulation, and stromal interactions, making it useful for vascular normalization and combination therapy studies in preclinical models.

Experimental Applications:

  • In vitro angiogenesis assays: tube formation, migration, sprouting

  • In vivo xenograft tumor vascular studies

  • Combination therapy evaluation

  • Resistance mechanism and compensatory pathway analysis

    fruquintinib-cas-1194506-26-7-images


Side Effects

In preclinical research, VEGFR inhibition by Fruquintinib demonstrates predictable laboratory effects:

  • Cell cycle arrest: slowing proliferation of endothelial and tumor cells

  • Apoptosis induction: caspase-mediated and mitochondrial pathway activation

  • Angiogenesis suppression: reduced tube formation and migration

  • Microenvironment modulation: altered tumor oxygenation, perfusion, and stromal interactions

  • Gene expression changes: downregulation of VEGF-A, cyclin D1, c-Myc, and angiogenesis-related genes

Laboratory Safety Guidelines:

  • Wear gloves, lab coat, and eye protection

  • Use fume hood; avoid skin contact and inhalation

  • Store at 2–8 °C, protected from light and moisture

  • Dispose of waste per institutional chemical safety protocols

Fruquintinib is strictly for laboratory research use only.


Keywords

Fruquintinib, VEGFR inhibitor, selective small molecule, preclinical oncology research, angiogenesis inhibition, tumor proliferation, tumor microenvironment modulation, high-purity research compound, laboratory research chemical, VEGFR-targeted agent


Shipping Guarantee

All shipments of Fruquintinib use validated cold-chain logistics to ensure compound integrity from warehouse to laboratory. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Express international couriers with full tracking and insurance are employed, guaranteeing safe and timely delivery. Additionally, our logistics team verifies handling conditions during transit to minimize exposure to heat, light, or moisture, ensuring reproducible research outcomes.


Trade Assurance

We guarantee the authenticity of Fruquintinib, with verified ≥99% purity and compliance with HPLC, MS, and NMR analytical standards. Each batch comes with a Certificate of Analysis (CoA) for verification. Our trade assurance policy provides replacement or refund in the rare event of deviation from listed specifications. This ensures research laboratories receive consistent, high-quality material for reproducible experimental results. Trade assurance also covers secure packaging and accurate labeling for safe global shipping.


Payment Support

We offer flexible and secure global payment options to support international research transactions. Accepted methods include PayPal, major credit cards (Visa, MasterCard, American Express), telegraphic transfer (T/T), and cryptocurrencies (USDT, Bitcoin, Ethereum). All transactions are protected by industry-standard encryption and verified gateways, ensuring confidentiality and fund security. For large or recurring orders, our payment support team can provide customized solutions and facilitate smooth procurement for research institutions.


Disclaimer

All products, including Fruquintinib, are intended strictly for laboratory research use only and are not for human or veterinary use. They are not drugs, medical devices, or diagnostic agents and should not be administered to humans or animals. Researchers must follow institutional biosafety and chemical safety guidelines during handling and disposal. The information provided is for scientific reference only and does not imply therapeutic efficacy, safety, or regulatory approval. Users are advised to conduct risk assessments, follow local regulations, and implement all standard laboratory precautions.

Additional information

Weight1.1 kg
Dimensions18 × 16 × 18 cm

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What is Fruquintinib used for?

Preclinical oncology research on VEGFR-mediated angiogenesis inhibition, tumor proliferation, and microenvironment modulation.

Is Fruquintinib a peptide?

No, it is a small-molecule VEGFR inhibitor.

What is the purity of Fruquintinib?

≥99%, verified via HPLC and MS.

How should it be stored?

Store at 2–8 °C, protected from light and moisture.

Which solvents is Fruquintinib soluble in?

DMSO and ethanol; slightly soluble in water.

Can it be used in in vivo models?

Yes, under approved preclinical protocols.

Does it come with documentation?

Each batch includes CoA and analytical verification.

Is bulk purchase or OEM available?

Yes, via research chemical suppliers in China.

Is it stable during storage?

Stable up to 24 months under recommended conditions.

Which research areas use Fruquintinib?

Angiogenesis assays, tumor proliferation studies, microenvironment research, preclinical oncology studies.

Can it be combined with other therapies?

Yes, commonly with chemotherapeutic or targeted agents.

What safety precautions are recommended?

Gloves, lab coat, and fume hood; avoid skin contact and inhalation.

Is it available from peptide wholesale China suppliers?

Yes, through international laboratory chemical distributors.

Can analogues be synthesized?

OEM services are available for analogues and derivatives.

Why is Fruquintinib valuable for research?

Selective VEGFR inhibition and ≥99% purity allow precise mechanistic studies on angiogenesis, tumor growth, and preclinical oncology pathways.


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