Erdafitinib (JNJ-42756493)

Name: Erdafitinib (JNJ-42756493)
Brand: Selleck Chemicals
SKU: S8401
Rating: 5 (5 reviews)

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.

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

Cancers (Basel), 2020, 26;12(6):E1366

PubMed: 32466597 ( click the link to review the publication )

Cancer Immunol Res, 2019, 7(9):1457-1471

PubMed: 31331945 ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104

PubMed: 31585938 ( click the link to review the publication )

J Exp Clin Cancer Res, 2019, 38(1):322

PubMed: 31331377 ( click the link to review the publication )

Clin Cancer Res, 2017, 10.1158/1078-0432.CCR-17-0478

PubMed: 28630215 ( click the link to review the publication )

1 Customer Review

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.

Purity & Quality Control

Choose Selective FGFR Inhibitors

Biological Activity

Description

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 BMC Cancer 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 BMC Cancer 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 BMC Cancer 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]	- Collapse 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]	- Collapse Animal Models: NMRI nu/nu female mice Dosages: 40 mg/kg Administration: by gavage (Only for Reference)

References

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 Download Erdafitinib (JNJ-42756493) SDF

Molecular Weight	446.54
Formula	C₂₅H₃₀N₆O₂
CAS No.	1346242-81-6
Storage	3 years-20°C powder 2 years-80°C 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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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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
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Bio Calculators

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The Serial Dilution Calculator Equation

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-09-01)

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

FGFR Signaling Pathway Map

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Erdafitinib (JNJ-42756493)