Description

Product Description

Pemigatinib, CAS 1513857-77-6, is a potent and selective inhibitor of fibroblast growth factor receptors FGFR1, FGFR2, and FGFR3. As a small-molecule kinase inhibitor, it has gained attention in preclinical oncology research for its ability to modulate FGFR-mediated signaling pathways, suppress aberrant cell proliferation, induce apoptosis, and interfere with oncogenic transformation. Pemigatinib’s high specificity enables mechanistic studies of FGFR-driven cancers, including cholangiocarcinoma, bladder carcinoma, and other malignancies with FGFR alterations.

In preclinical models, Pemigatinib binds the ATP-binding pocket of FGFR1–3, preventing autophosphorylation and subsequent downstream signaling through MAPK, PI3K/AKT, and STAT pathways. This leads to reduced proliferation, altered cell-cycle progression, apoptosis induction, and modulation of tumor-relevant gene expression. Its tablet formulation allows precise in vitro dissolution studies, pharmacokinetic investigations, and preclinical in vivo dosing in animal models, providing a reproducible platform for FGFR-targeted oncology research.

Pemigatinib is used extensively to explore mechanisms of FGFR-mediated oncogenic signaling, drug resistance pathways, combination therapy effects, and off-target kinase activity. Its stability as a solid oral dosage form facilitates accurate dosing in cell culture, xenograft models, and pharmacodynamic assays. Researchers can leverage Pemigatinib to dissect FGFR-dependent tumorigenesis, evaluate targeted therapy responses, and understand FGFR pathway modulation in the context of drug development.

Mechanistic studies reveal that Pemigatinib inhibits FGFR autophosphorylation, resulting in downstream blockade of RAS/MAPK, PI3K/AKT, and STAT signaling. This causes G1-phase cell-cycle arrest, suppression of tumor-promoting gene transcription, and induction of intrinsic apoptosis pathways. Its high-purity tablet format ensures reliable experimental outcomes for pharmacological, biochemical, and molecular investigations.

In addition to monotherapy preclinical studies, Pemigatinib is employed in combination assays with chemotherapeutic agents, immune modulators, or other kinase inhibitors to study synergistic or antagonistic effects. Researchers can also examine acquired resistance mechanisms, such as FGFR gatekeeper mutations, receptor amplification, or compensatory pathway activation.

Product Specifications

Mechanism of Action

FGFR Inhibition

Pemigatinib selectively inhibits FGFR1, FGFR2, and FGFR3 by binding the ATP-binding site of the receptor kinases. This prevents autophosphorylation and disrupts downstream signaling cascades responsible for cell proliferation, survival, and differentiation.

Downstream Signaling Modulation

• MAPK pathway: Reduced ERK phosphorylation and decreased transcription of proliferation-promoting genes.

• PI3K/AKT pathway: Inhibition of survival signaling, promoting apoptosis.

• STAT signaling: Impairment of oncogenic transcription factor activation.

Cell-Cycle Arrest and Apoptosis

• Induces G1-phase cell-cycle arrest, reducing proliferation.

• Activates intrinsic apoptosis pathways via mitochondrial depolarization and caspase activation.

• Modulates tumor-relevant gene expression associated with FGFR signaling.

Combination and Resistance Studies

• Used in combination assays with chemotherapeutic agents and other kinase inhibitors.

• Facilitates study of acquired resistance mechanisms, including FGFR mutations and compensatory signaling.

• Enables exploration of FGFR pathway dependency in cancer models.

  

Side Effects

Cellular Effects:

• FGFR pathway inhibition leads to G1-phase arrest

• Reduced cell proliferation

• Potential induction of ROS in sensitive cell lines

Apoptotic Effects:

• Activation of intrinsic apoptosis via mitochondrial pathways

• Caspase-dependent cell death

• Modulation of p53 and other transcriptional regulators

Laboratory Handling:

• Tablets should be handled with PPE

• Strictly for laboratory research; cytotoxic and kinase-inhibiting properties require caution

Keywords

Pemigatinib, INCB054828, FGFR inhibitor, FGFR1/2/3 inhibitor, FGFR signaling, targeted oncology research, cell proliferation studies, apoptosis assays, oncogenic pathway studies, combination therapy research, resistance mechanism modeling, high-purity research chemical, factory small-molecule supplier, peptide wholesale China, China chemical manufacturer, OEM & bulk production, laboratory research reagent

Shipping Guarantee

All Pemigatinib shipments of Pemigatinib tablets are handled using validated cold-chain or controlled temperature logistics to maintain compound stability. Packages are sealed with protective wrapping and shipped via express international couriers with tracking and insurance.

Trade Assurance

We Pemigatinib guarantee product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, NMR). Each batch is supplied with a Certificate of Analysis (CoA). Replacement or refund is provided for any deviation from listed specifications.

Payment Support

Flexible global payment options: PayPal, major credit cards (Visa, MasterCard, American Express), T/T, USDT, Bitcoin, Ethereum. All transactions are encrypted and verified to ensure confidentiality and security.

Disclaimer

Pemigatinib is supplied strictly for laboratory research. Not for human or veterinary use. Researchers must adhere to institutional safety guidelines. Supplier assumes no liability for misuse.

References

• PubChem: Pemigatinib (CID 71478285)

• ChEMBL Database: Pemigatinib Bioactivity Summary (CHEMBL4325316)

• DrugBank: Pemigatinib – DB15155

• PubMed ID 30850153: Preclinical studies of Pemigatinib in FGFR-driven cancers

• IUPHAR/BPS Guide to Pharmacology: FGFR inhibitors