Erdafitinib (JNJ-42756493)

Catalog No.S8401

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.

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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

    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.
Targets
FGFR [1]
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

Cell Research:

[2]

+ Expand
  • 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]

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

Solubility (25°C)

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

Chemical Information

Molecular Weight 446.54
Formula

C25H30N6O2

CAS No. 1346242-81-6
Storage powder
Synonyms N/A

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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.

Handling Instructions

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Related Antibodies

FGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID