Description

Product Description

Anlotinib Hydrochloride is a synthetic, small-molecule tyrosine kinase inhibitor (TKI) known for its broad-spectrum inhibition of angiogenic and oncogenic pathways. It demonstrates significant activity against vascular endothelial growth factor receptors (VEGFR1/2/3), fibroblast growth factor receptors (FGFR1-4), platelet-derived growth factor receptors (PDGFRα/β), and the stem cell factor receptor c-Kit. This broad inhibitory profile makes it a key compound in cancer biology and pharmacological mechanism research.

Anlotinib Hydrochloride functions primarily by interrupting the VEGF and FGF signaling cascades, essential pathways responsible for tumor angiogenesis and metastasis. By targeting these receptors, Anlotinib effectively suppresses endothelial cell proliferation, migration, and new vessel formation—thereby starving tumors of essential oxygen and nutrients. In preclinical cancer models, it demonstrates potent anti-angiogenic and anti-tumor properties with minimal off-target cytotoxicity compared to earlier TKIs.

Molecular Features and Research Relevance

Chemically, Anlotinib Hydrochloride possesses high lipophilicity, ensuring efficient cellular uptake and sustained receptor occupancy. This contributes to prolonged kinase inhibition in in vitro and in vivo research systems. Researchers have extensively employed it to explore mechanisms of anti-angiogenesis, tumor hypoxia adaptation, and TKI resistance.

In addition to anti-angiogenic activity, Anlotinib modulates downstream signaling cascades such as PI3K/Akt, ERK/MAPK, and STAT3—key pathways that regulate cell proliferation, apoptosis, and autophagy. Consequently, Anlotinib is often included in studies focused on signal transduction, gene expression profiling, and combined therapeutic modeling.

Applications in Research

Anlotinib Hydrochloride is utilized across various oncology research domains:

• Angiogenesis studies: Inhibits VEGF-induced endothelial cell proliferation and migration.

• Signal transduction research: Modulates FGFR and PDGFR-dependent downstream cascades.

• Resistance mechanism exploration: Investigates adaptive responses in tumor microenvironments to chronic kinase inhibition.

• Combination therapy evaluation: Enhances efficacy of chemotherapeutics, radiotherapy, and immune checkpoint inhibitors in preclinical studies.

• Tumor metabolism studies: Suppresses glycolysis and hypoxia signaling pathways in solid tumor cell lines.

These applications make Anlotinib Hydrochloride a versatile compound for translational oncology and pharmacodynamics research.

Pharmacological Insights

In cancer cell models, Anlotinib demonstrates dose-dependent inhibition of proliferation and migration. It effectively reduces phosphorylated VEGFR2 and FGFR3 levels, impairing endothelial tube formation. Furthermore, it induces G2/M cell cycle arrest and promotes apoptosis via activation of caspase-3 and downregulation of anti-apoptotic proteins such as Bcl-2.

Experimental data indicate that long-term exposure to Anlotinib may alter tumor metabolism and enhance immune recognition, offering valuable insights for next-generation therapeutic development.

Experimental Usage

• In vitro: Effective in endothelial and tumor cell assays at micromolar concentrations.

• In vivo: Commonly used in xenograft and angiogenesis mouse models for mechanism studies.

• Analytical tools: LC-MS and HPLC methods confirm compound integrity and purity.

Researchers often pair Anlotinib with growth factors, receptor agonists, or genetic knockdowns to delineate pathway interactions.

Summary

Anlotinib Hydrochloride is a high-purity, multi-target kinase inhibitor indispensable for studying tumor angiogenesis, signaling cross-talk, and resistance mechanisms. Its ability to modulate multiple oncogenic pathways simultaneously positions it as a cornerstone reagent in molecular oncology and preclinical pharmacology.

Product Specifications

Mechanism of Action

Anlotinib Hydrochloride inhibits several receptor tyrosine kinases (RTKs) critical for angiogenesis and tumor progression. It blocks ATP binding to VEGFR, FGFR, and PDGFR kinase domains, preventing receptor phosphorylation and downstream signaling activation.

VEGFR Inhibition

VEGFR1-3 play essential roles in blood vessel formation and endothelial cell migration. Anlotinib’s inhibition of VEGFR2 results in reduced endothelial proliferation, migration, and vascular permeability. This leads to suppression of neovascularization and inhibition of tumor growth in research models.

FGFR and PDGFR Modulation

The FGFR signaling pathway supports fibroblast proliferation and tissue remodeling within the tumor microenvironment. Anlotinib disrupts this pathway, decreasing fibroblast activation and extracellular matrix deposition. Its PDGFR inhibition complements anti-angiogenic effects by reducing pericyte recruitment and vessel stability.

Downstream Pathway Effects

By targeting multiple receptors, Anlotinib suppresses:

• PI3K/Akt/mTOR signaling: Reduces cell survival and metabolic activity.

• Ras/Raf/MEK/ERK cascade: Inhibits proliferation and mitogenic signaling.

• STAT3 activation: Attenuates inflammatory cytokine production and tumor immune evasion.

This multi-pathway inhibition establishes a strong preclinical rationale for Anlotinib in anti-tumor mechanism exploration.

Apoptosis and Cell Cycle Regulation

Anlotinib induces apoptosis in cancer cell lines by modulating Bax/Bcl-2 ratios, activating caspase-9, and cleaving PARP. It also halts cell cycle progression at G2/M, providing a model to study checkpoint regulation and DNA damage response in oncogenic contexts.

Resistance and Adaptive Mechanisms

Research indicates that chronic exposure to Anlotinib may upregulate alternative pro-angiogenic signals (e.g., HIF-1α, VEGF-A), leading to adaptive resistance. These features make it valuable for investigating resistance biomarkers and designing second-line TKI strategies.

Immunomodulatory Role

Anlotinib may reshape the tumor immune landscape by decreasing regulatory T-cell infiltration and enhancing cytotoxic T-cell activity in experimental tumor models. This emerging research direction is critical for understanding combinational effects with immunotherapies.

Side Effects

In laboratory settings, Anlotinib Hydrochloride may induce concentration-dependent cytotoxic effects such as:

• Mitochondrial dysfunction and oxidative stress.

• Cell cycle arrest and altered proliferation in endothelial and tumor cells.

• Metabolic perturbations in glycolysis and oxidative phosphorylation studies.

• Increased apoptotic signaling, observed through caspase activation assays.

Proper handling and protective equipment are required during use. The compound should not be used for human or veterinary purposes.

Keywords

Anlotinib Hydrochloride, CAS 1360460-82-7, multi-target TKI, VEGFR inhibitor, PDGFR blocker, FGFR modulation, angiogenesis research, tumor signaling pathway, anti-angiogenic compound, oncology reagent, high purity kinase inhibitor

Shipping Guarantee

All Anlotinib Hydrochloride shipments are handled using validated cold-chain logistics to preserve compound integrity. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with full tracking and insurance coverage.

Trade Assurance

We Anlotinib Hydrochloride ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, and NMR). Each batch is supplied with a Certificate of Analysis (CoA). Our trade assurance policy guarantees replacement or refund for any deviation from listed specifications.

Payment Support

We Anlotinib Hydrochloride provide flexible and secure global payment options to support international research transactions. Accepted payment 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 payment gateways to ensure confidentiality and fund security.

Disclaimer

All Anlotinib Hydrochloride products are intended for laboratory research use only and not for human or veterinary use. They are not drugs, medical devices, or diagnostic tools. Researchers must handle materials according to institutional chemical and biosafety regulations. The provided information is for scientific reference only and does not imply therapeutic efficacy or regulatory approval.