Erdafitinib (JNJ-42756493)

Catalog No.S8401

For research use only.

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 (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.

Erdafitinib (JNJ-42756493) Chemical Structure

CAS No. 1346242-81-6

Selleck's Erdafitinib (JNJ-42756493) has been cited by 18 publications

Purity & Quality Control

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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 (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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BA/F3 MnnwSpVv[3Srb36gZZN{[Xl? NYD0fGNzOjRiaILz MWrJcohq[mm2aX;uJI9nKE[JRmKzJEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[2WubDDwdo9tcW[ncnH0bY9vKGmwIHHid4Vv[2Vib3[gcY92e2ViSVyzJIFnfGW{IEK0JIhzeyCkeTDBcIFu[XJiYnz1[UBie3OjeTygTWM2OCB;IECuNFE2QDVizszNMi=> NYLZSGdrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzV2NUO3Ok8oRkOqRV3CUFww[T5?
BA/F3 Mln2SpVv[3Srb36gZZN{[Xl? NEP4e3ozPCCqcoO= NELHUWhKdmirYnn0bY9vKG:oIF\HSnIyKCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEBxem:uaX\ldoF1cW:wIHnuJIFje2WwY3Wgc4YhdW:3c3WgTWw{KGGodHXyJFI1KGi{czDifUBCdGGvYYKgZox2\SCjc4PhfUwhUUN3MDC9JFAvODh|MUig{txONg>? MlnEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|U1PTN5Nj:nQmNpTU2ETEyvZV4>
BA/F3 NGSxOmVHfW6ldHnvckBie3OjeR?= M4jWcVI1KGi{cx?= MofRTY5pcWKrdHnvckBw\iCYRVfGVlIhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJJBzd2yrZnXyZZRqd25iaX6gZYJ{\W6lZTDv[kBud3W|ZTDJUFMh[W[2ZYKgNlQhcHK|IHL5JGFt[W2jcjDicJVmKGG|c3H5MEBKSzVyIE2gN{4{OTF|MTFOwG0v NHHlT|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PTR3M{e2M{c,S2iHTVLMQE9iRg>?
Assay
Methods Test Index 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, 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 Research:

[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.

  • (Only for Reference)
Animal Research:

[2]

  • 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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04330248 Suspended 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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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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