Erdafitinib

Catalog No.S8401 Batch:S840102

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Technical Data

Formula

C25H30N6O2
Molecular Weight 446.54 CAS No. 1346242-81-6
Solubility (25°C)* In vitro DMSO 89 mg/mL (199.31 mM)
Ethanol 17 mg/mL (38.07 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.)

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Biological Activity

Description Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.
Targets
FGFR [1] RET [3] CSF-1R [3] PDGFR [3] Kit [3] View More
In vitro

JNJ-42756493 is a potent, oral pan-FGFR tyrosine kinase inhibitor with half-maximal inhibitory concentration values in the low nanomolar range for all members of the FGFR family (FGFR1 to FGFR4), with minimal activity on vascular endothelial growth factor receptor (VEGFR) kinases compared with FGFR kinases (approximately 20-fold potency difference). In vitro, the proliferation of cells treated with JNJ-42756493 is decreased, associated with increased apoptotic death and decreased cell survival[2].
In vivo

In vivo, growth of NCI-H716 tumors is delayed by 5 days by drug treatment alone, although when drug delivery is stopped the relative tumor volume increased compared to control[2]. JNJ-42756493 shows favorable drug like properties and displays a high distribution to lung, liver and kidney tissue. JNJ-42756493 is well tolerated at efficacious doses and results in potent dose-dependent antitumor activity accompanied by pharmacodynamic modulation of tumor FGFR and downstream pathway components[1].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    HCT116, HCA7, Caco2 and NCI-H716 cells

  • Concentrations

    --

  • Incubation Time

    72 h

  • Method

    The effect of varying drug concentrations on cell growth and survival is evaluated at 72 h using sulforhodamine B (SRB) assay for the adherent cells (HCT116, HCA7, Caco2) and trypan blue dye exclusion for the suspension cells, NCI-H716.
Animal Study:

[2]
  • Animal Models

    NMRI nu/nu female mice

  • Dosages

    40 mg/kg

  • Administration

    by gavage

Customer Product Validation

, , Clin Cancer Res, 2017, 23(18):5527-5536

Selleck's Erdafitinib has been cited by 35 publications

FGFR inhibition augments anti-PD-1 efficacy in murine FGFR3-mutant bladder cancer by abrogating immunosuppression [ J Clin Invest, 2024, 134(2)e169241] PubMed: 38226620
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] PubMed: 37377403
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] PubMed: 37377403
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] PubMed: 37377403
"Proteotranscriptomic analysis of advanced colorectal cancer patient derived organoids for drug sensitivity prediction" [ J Exp Clin Cancer Res, 2023, 42(1):8] PubMed: 36604765
18F-FDG PET as an imaging biomarker for the response to FGFR-targeted therapy of cancer cells via FGFR-initiated mTOR/HK2 axis [ Theranostics, 2022, 12(14):6395-6408] PubMed: 36168616
FGFR blockade boosts T cell infiltration into triple-negative breast cancer by regulating cancer-associated fibroblasts [ Theranostics, 2022, 12(10):4564-4580] PubMed: 35832090
Targeting PEA3 transcription factors to mitigate small cell lung cancer progression [ Oncogene, 2022, 10.1038/s41388-022-02558-6] PubMed: 36509998
Intranasal delivery of a small-molecule ErbB inhibitor promotes recovery from acute and late-stage CNS inflammation [ JCI Insight, 2022, 7(7)e154824] PubMed: 35393953
Immunomodulation via FGFR inhibition augments FGFR1 targeting T-cell based antitumor immunotherapy for head and neck squamous cell carcinoma [ Oncoimmunology, 2022, 11(1):2021619] PubMed: 35003900

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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.

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