Fisogatinib (BLU-554)

Catalog No.S8503 Batch:S850301

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Technical Data

Formula

C24H24Cl2N4O4
Molecular Weight 503.38 CAS No. 1707289-21-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (198.65 mM)
Ethanol 2 mg/mL (3.97 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Fisogatinib (BLU-554) is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM.
Targets
FGFR4 [1]
(Cell-free assay)
5 nM
In vitro

BLU-554 exploits a unique interaction with FGFR4 to confer potency and selectivity
In vivo

BLU-554 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models[1].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    ST8814 resistant cells

  • Concentrations

    1 µM

  • Incubation Time

    4 h

  • Method

    ST8814 resistant cells were treated with DMSO or BLU-554 at 1 µM for 4 hrs.
Animal Study:

[3]
  • Animal Models

    Male FVB/NRj mice

  • Dosages

    10 mg/kg

  • Administration

    p.o.

Selleck's Fisogatinib (BLU-554) has been cited by 7 publications

FGF19-Induced Inflammatory CAF Promoted Neutrophil Extracellular Trap Formation in the Liver Metastasis of Colorectal Cancer [ Adv Sci (Weinh), 2023, 10(24):e2302613] PubMed: 37345586
Fibroblast growth factor receptor 4 promotes glioblastoma progression: a central role of integrin-mediated cell invasiveness [ Acta Neuropathol Commun, 2022, 10(1):65] PubMed: 35484633
BLU-554, A selective inhibitor of FGFR4, exhibits anti-tumour activity against gastric cancer in vitro [ Biochem Biophys Res Commun, 2022, 595:22-27] PubMed: 35093636
EGFR activation limits the response of liver cancer to lenvatinib [ Nature, 2021, 595(7869):730-734] PubMed: 34290403
Activation of receptor tyrosine kinases mediates acquired resistance to MEK inhibition in malignant peripheral nerve sheath tumors [ Cancer Res, 2020, canres.1992.2020] PubMed: 33203698
Chemosensitivity of Patient-Derived Cancer Stem Cells Identifies Colorectal Cancer Patients with Potential Benefit from FGFR Inhibitor Therapy [ Cancers (Basel), 2020, 12(8):E2010] PubMed: 32708005
Protein tyrosine kinase 2: a novel therapeutic target to overcome acquired EGFR-TKI resistance in non-small cell lung cancer [ Respir Res, 2019, 20(1-:270] PubMed: 31791326

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.