Home Angiogenesis FGFR inhibitor - c-RET inhibitor - CSF-1R inhibitor - PDGFR inhibitor - VEGFR inhibitor - Apoptosis related activator - c-Kit inhibitor Erdafitinib For research use only.

Erdafitinib

Synonyms: JNJ-42756493

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.

Erdafitinib Chemical Structure

Erdafitinib Chemical Structure

CAS: 1346242-81-6

Selleck's Erdafitinib has been cited by 32 publications

Purity & Quality Control

Batch: Purity: 99.94%
99.94

Products often used together with Erdafitinib

Pemigatinib

Erdafitinib and Pemigatinib are approved by FDA for their use in the treatment of FGFR3-mutated urothelial carcinoma and FGFR2-fusion cholangiocarcinoma, respectively.

Krook MA, et al. Br J Cancer. 2021 Mar;124(5):880-892.

Alpelisib (BYL719)

Erdafitinib and Alpelisib combined with the canonical cytotoxic agents result in variable synergistic, additive, and antagonistic effects in neuroblastoma (NB) cell lines.

Holzhauser S, et al. Int J Oncol. 2021 Feb;58(2):211-225.

Navitoclax (ABT-263)

Erdafitinib and Navitoclax induce potent apoptosis in urothelial carcinoma cell lines without FGFR mutation.

Ohtsu A, et al. Cancer Res (2021) 81 (13_Supplement): 1928.

Idasanutlin (RG7388)

Erdafitinib and Idasanutlin exert a synergistic effect on viability, apoptosis, and clonogenicity in one WDLPS and two DDLPS cell lines.

Dadone-Montaudie B, et al. Cancers (Basel). 2020 Oct 20;12(10):3058.

AZD4547

Erdafitinib and AZD4547 not only inhibit cell proliferation but also reduce the 18F-FDG uptake in NCI-H1581 cells.

Jiang Y, et al. Theranostics. 2022 Aug 29;12(14):6395-6408.

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BA/F3 Function assay 24 hrs Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed as decrease in cell proliferation in absence of mouse IL3 after 24 hrs by Alamar blue assay, IC50 = 0.01585 μM. ChEMBL
BA/F3 Function assay 24 hrs Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed as decrease in cell proliferation in absence of mouse IL3 after 24 hrs by Alamar blue assay, IC50 = 0.08318 μM. ChEMBL
BA/F3 Function assay 24 hrs Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed as decrease in cell proliferation in absence of mouse IL3 after 24 hrs by Alamar blue assay, IC50 = 3.31131 μM. ChEMBL
Click to View More Cell Line Experimental Data

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] Click to View More Targets
In vitro
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot FGFR2 / p-FGFR PARP / Cleaved PARP / AKT / p-AKT / p-ERK / ERK2 26675289
Growth inhibition assay Cell viability 26675289
In Vivo
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].
Animal Research Animal Models NMRI nu/nu female mice
Dosages 40 mg/kg
Administration by gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05567185 Recruiting Urinary Bladder Neoplasms|Receptors Fibroblast Growth Factor Janssen Pharmaceutical K.K. March 3 2023 Phase 1
NCT05316155 Recruiting Urinary Bladder Neoplasms|Receptors Fibroblast Growth Factor Janssen Research & Development LLC April 11 2022 Phase 1
NCT05052372 Terminated Bladder Cancer|Urothelial Carcinoma|Transitional Cell Carcinoma|Platinum-Resistant Urothelial Carcinoma|Bladder Urothelial Carcinoma|FGFR Mutation|FGFR2 Gene Mutation|FGFR3 Gene Mutation|FGFR2 Amplification|Locally Advanced Urothelial Carcinoma|Metastatic Urothelial Carcinoma|Refractory Bladder Carcinoma|Refractory Bladder Urothelial Carcinoma xCures November 21 2021 --
NCT04330248 Completed Healthy Johnson & Johnson Pharmaceutical Research & Development L.L.C. March 31 2020 Phase 1
NCT04083976 Active not recruiting Advanced Solid Tumor Janssen Research & Development LLC November 20 2019 Phase 2

Chemical lnformation & Solubility

Molecular Weight 446.54 Formula

C25H30N6O2
CAS No. 1346242-81-6 SDF Download Erdafitinib SDF
Smiles CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (199.31 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 89 mg/mL

Water : Insoluble


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In vivo
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