FGFR4-IN-1 Selective Inhibitor: Research Use Guidelines

FGFR4-IN-1 is a selective small-molecule inhibitor of fibroblast growth factor receptor 4 (FGFR4), supplied by Aladdin Scientific (SKU F649982) for use in preclinical research investigating FGFR4-driven signaling pathways and related oncological models.

Product Name

FGFR4-IN-1

SKU

F649982

Primary Target

Fibroblast Growth Factor Receptor 4 (FGFR4)

Compound Class

Selective kinase inhibitor (small molecule)

Reference Catalog Number

MCE HY-100631

Recommended Storage

-20 °C, protected from light and moisture (verify with product datasheet)

Application

In vitro and in vivo FGFR4 inhibition research; oncology signaling studies

Background: FGFR4 Biology and Therapeutic Relevance

Fibroblast growth factor receptor 4 (FGFR4) is a receptor tyrosine kinase belonging to the FGFR family (FGFR1–4). Upon binding its cognate fibroblast growth factors (FGFs), FGFR4 activates downstream signaling cascades including the RAS/MAPK, PI3K/AKT, and STAT3 pathways, regulating cell proliferation, differentiation, survival, and metabolism.

Aberrant FGFR4 activity—arising from gene amplification, activating mutations, or overexpression—has been implicated in multiple malignancies, most notably hepatocellular carcinoma (HCC), rhabdomyosarcoma, and breast cancer. FGFR4 therefore represents a validated oncology target, and selective inhibitors are important research tools for delineating its precise role in disease models.

Review flag: Specific cancer types and mechanistic details should be verified against peer-reviewed literature before inclusion in publications.

Compound Profile and Selectivity

FGFR4-IN-1 is designed as a selective inhibitor of FGFR4 relative to other FGFR family members (FGFR1, FGFR2, FGFR3). Selectivity for FGFR4 over closely related kinases is a key attribute that makes this compound valuable for dissecting FGFR4-specific contributions to cellular phenotypes without confounding pan-FGFR inhibition effects.

The compound is referenced under MCE catalog number HY-100631. Researchers are advised to consult the product-specific datasheet (available from Aladdin Scientific at SKU F649982) for confirmed biochemical potency data (IC₅₀ values), selectivity panel results, and molecular weight/formula information, as these parameters are subject to lot-specific quality control testing.

Review flag: Exact IC50 values, molecular weight, and molecular formula are not provided in the source material and must be retrieved from the official product datasheet or primary literature before citing.

Handling, Reconstitution, and Storage Guidelines

Reconstitution: FGFR4-IN-1 is typically supplied as a lyophilized solid or powder. For stock solution preparation, dissolve the compound in dimethyl sulfoxide (DMSO) to yield a concentrated stock (e.g., 10–50 mM). Ensure complete dissolution by vortexing and brief sonication if necessary. Always prepare fresh working dilutions in aqueous cell culture media immediately before use; the final DMSO concentration in assay wells should generally not exceed 0.1% (v/v) to avoid cytotoxic artifacts.

Storage: Store the compound at −20 °C in a tightly sealed container, protected from light and moisture. Avoid repeated freeze–thaw cycles by preparing single-use aliquots. Confirm specific storage conditions on the Aladdin Scientific product datasheet for SKU F649982.

Safety: Handle in accordance with standard laboratory chemical safety practices. Consult the Safety Data Sheet (SDS) provided with the product. Avoid inhalation of dust and contact with skin or eyes. Dispose of waste in accordance with local regulations.

Review flag: Solubility values and recommended stock concentrations are not confirmed in source material; verify against product datasheet before use.

Experimental Design and Best Practices

Cell-Based Assays: When using FGFR4-IN-1 in cellular models, select cell lines with confirmed FGFR4 expression or overexpression (e.g., hepatocellular carcinoma lines). Include appropriate vehicle controls (DMSO at matched concentration), positive controls (a validated pan-FGFR inhibitor if available), and negative controls. Assess cell viability, receptor phosphorylation (pFGFR4 Y642 or equivalent site), and downstream pathway markers (pFRS2, pERK, pAKT) to confirm on-target activity.

Dose–Response Analysis: Perform multi-point dose–response experiments across at least 8 concentrations (typically 0.1 nM–10 µM range, adjusted based on the compound's IC₅₀) to determine EC₅₀/IC₅₀ values in the chosen model system. Confirm that observed effects are reversible or compete with FGF ligand stimulation to substantiate FGFR4 selectivity.

In Vivo Studies: Formulation for in vivo administration typically requires a vehicle such as 5% DMSO in corn oil or PEG400-based formulations. Consult current literature and the product datasheet for pharmacokinetic guidance. Institutional animal care and use committee (IACUC) approval is required before any in vivo experiment.

Review flag: Specific recommended concentrations, formulation vehicles, and pharmacokinetic parameters are not confirmed in source material; these must be sourced from primary literature and verified experimentally.

Quality Control and Regulatory Considerations

Purity and QC: Each lot of FGFR4-IN-1 (SKU F649982) is subject to quality control testing. Researchers should request and review the Certificate of Analysis (CoA) for the specific lot received, confirming purity (typically ≥98% by HPLC), identity (NMR or HRMS), and appearance prior to experimental use.

Research Use Only: FGFR4-IN-1 is supplied strictly for research purposes and is not approved, validated, or intended for use in diagnostic procedures, therapeutic applications, or any clinical setting in humans or animals without appropriate regulatory authorization.

Documentation: Maintain complete records of lot number, storage conditions, reconstitution date, and working concentrations for reproducibility and regulatory traceability. Reference both the Aladdin Scientific SKU (F649982) and the MCE catalog number (HY-100631) in experimental records and publications to ensure unambiguous compound identification.

Frequently asked questions

What is FGFR4-IN-1 and what does it inhibit?

FGFR4-IN-1 is a selective small-molecule inhibitor targeting fibroblast growth factor receptor 4 (FGFR4), a receptor tyrosine kinase involved in cell proliferation, differentiation, and survival signaling. It is used as a research tool to study FGFR4-dependent pathways in cancer and other disease models.

How should I dissolve and store FGFR4-IN-1?

FGFR4-IN-1 is typically dissolved in DMSO to prepare a concentrated stock solution. Store the compound at −20 °C in a sealed, light-protected container and prepare single-use aliquots to prevent degradation from repeated freeze–thaw cycles. Always consult the lot-specific Certificate of Analysis and product datasheet (SKU F649982) for confirmed solubility and storage instructions.

What controls should I include when using FGFR4-IN-1 in cell-based assays?

Include a vehicle control using the same concentration of DMSO as in treated samples, a positive control with a validated reference inhibitor if available, and confirm on-target activity by measuring FGFR4 phosphorylation and downstream markers such as pFRS2 and pERK. Using FGFR4-expressing cell lines alongside FGFR4-negative lines can further validate selectivity.

Is FGFR4-IN-1 suitable for in vivo studies?

FGFR4-IN-1 can be used in preclinical in vivo research, but appropriate formulation (such as DMSO/corn oil or PEG400-based vehicles) and pharmacokinetic validation are required. All in vivo experiments must be conducted under approved institutional animal care protocols (IACUC). Consult the product datasheet and primary literature for formulation guidance.

Where can I find purity and identity data for my lot of FGFR4-IN-1?

Lot-specific purity and identity data are available in the Certificate of Analysis (CoA) provided with each shipment of FGFR4-IN-1 (SKU F649982). You may also contact Aladdin Scientific customer service to request a CoA for your specific lot number.

References

1. MedChemExpress (MCE) Product Page: FGFR4-IN-1, Catalog No. HY-100631. Retrieved from MedChemExpress website.
2. Aladdin Scientific Product Page: FGFR4-IN-1, SKU F649982. Aladdin Scientific, Shanghai.
3. Katoh M. Fibroblast growth factor receptors as treatment targets in clinical oncology. Nat Rev Clin Oncol. 2019;16(2):105-122. doi:10.1038/s41571-018-0115-y

Products are supplied for research and development use only. Not for use in humans, animals, diagnosis, or therapy.