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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Cited by 1 Publication

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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.
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
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02699606 Recruiting Neoplasm Janssen Research & Development LLC July 8 2016 Phase 2
NCT03210714 Recruiting Advanced Malignant Solid Neoplasm|Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma|Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma|FGFR1 Gene Mutation|FGFR2 Gene Mutation|FGFR3 Gene Mutation|FGFR4 Gene Mutation|Histiocytosis|Low Grade Glioma|Malignant Glioma|Recurrent Central Nervous System Neoplasm|Recurrent Childhood Ependymoma|Recurrent Childhood Malignant Germ Cell Tumor|Recurrent Childhood Medulloblastoma|Recurrent Childhood Non-Hodgkin Lymphoma|Recurrent Childhood Rhabdomyosarcoma|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Recurrent Hepatoblastoma|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Solid Neoplasm|Recurrent Neuroblastoma|Recurrent Osteosarcoma|Refractory Central Nervous System Neoplasm|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Solid Neoplasm|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Rhabdoid Tumor|Stage III Soft Tissue Sarcoma AJCC v7|Stage IV Soft Tissue Sarcoma AJCC v7|Wilms Tumor National Cancer Institute (NCI) November 6 2017 Phase 2
NCT03473743 Recruiting Urothelial Carcinoma Janssen Research & Development LLC April 5 2018 Phase 1|Phase 2
NCT03587363 Not yet recruiting Hepatic Impairment Janssen Research & Development LLC October 31 2018 Phase 1
NCT03547037 Recruiting Neoplasm Janssen Pharmaceutical K.K. August 31 2018 Phase 1
NCT02421185 Active not recruiting Carcinoma Hepatocellular Janssen Research & Development LLC May 25 2015 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