Erdafitinib (JNJ-42756493)

For research use only.

Catalog No.S8401

5 publications

Erdafitinib (JNJ-42756493) Chemical Structure

Molecular Weight(MW): 446.54

Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET, CSF-1R, PDGFR-α/PDGFR-β, FLT4, KIT and VEGFR-2 and induces cellular apoptosis.

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Selleck's Erdafitinib (JNJ-42756493) has been cited by 5 publications

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  • E, Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 μmol/L BGJ398 assessed by immunoblotting. FGFR inhibitors: AZD4547, BGJ398, and JNJ-42756493

    Clin Cancer Res, 2017, 23(18):5527-5536. Erdafitinib (JNJ-42756493) purchased from Selleck.

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Biological Activity

Description Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET, CSF-1R, PDGFR-α/PDGFR-β, FLT4, KIT and VEGFR-2 and induces cellular apoptosis.
Targets
FGFR [1]
()
RET [3]
()
CSF-1R [3]
()
PDGFR [3]
()
Kit [3]
()
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].

Assay
Methods Test Index PMID
Western blot
FGFR2 / p-FGFR ; 

PubMed: 26675289     


Immunoblot analysis of FGFR2 after 72 h treatment. β-actin was used as loading control. Blots shown are representative for one of two independent experiments.

PARP / Cleaved PARP / AKT / p-AKT / p-ERK / ERK2 ; 

PubMed: 26675289     


Immunoblotting for (cleaved)PARP and downstream signaling molecules after 72 h drug incubation. β-actin served as loading control. Blots shown are representative for two independent experiments

26675289
Growth inhibition assay
Cell viability; 

PubMed: 26675289     


Effect of different concentrations FGFR inhibitor for 72 h incubation on cell survival. Data = means ± SEM from three independent experiments performed in triplicate. ∗Significantly different from control conditions at the appropriate drug concentrations (p < 0.05; Tukey)

26675289
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

Cell Research:

[2]

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  • 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.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: NMRI nu/nu female mice
  • Dosages: 40 mg/kg
  • Administration: by gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 89 mg/mL (199.31 mM)
Water Insoluble
Ethanol '''89 mg/mL

* 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.

Chemical Information

Molecular Weight 446.54
Formula

C25H30N6O2

CAS No. 1346242-81-6
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04330248 Recruiting Drug: Erdafitinib|Drug: Rifampin Healthy Johnson & Johnson Pharmaceutical Research & Development L.L.C. April 3 2020 Phase 1
NCT04083976 Recruiting Drug: Erdafitinib Advanced Solid Tumor Janssen Research & Development LLC November 20 2019 Phase 2
NCT03547037 Recruiting Drug: JNJ-63723283|Drug: Erdafitinib Neoplasm Janssen Pharmaceutical K.K. August 31 2018 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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FGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID