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Erdafitinib

Catalog No. T3726 CAS 1346242-81-6

Synonyms: JNJ-42756493

Erdafitinib (JNJ-42756493) is a quinoxaline derivative compound, acts on FGFR1/2/3/4.

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Erdafitinib, CAS 1346242-81-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 97.00
50 mg	In stock	$ 155.00
100 mg	In stock	$ 238.00
500 mg	In stock	$ 588.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.07%

Purity: 99.04%

Purity: 99.01%

Purity: 98.62%

Purity: 96.66%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Erdafitinib (JNJ-42756493) is a quinoxaline derivative compound, acts on FGFR1/2/3/4.
Targets&IC50	FGFR4:5.7 nM, FGFR3:3.0nM, FGFR1:1.2 nM, FGFR2:2.5nM
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].
Cell Research	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)

Synonyms	JNJ-42756493
Molecular Weight	446.54
Formula	C25H30N6O2
CAS No.	1346242-81-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 15 mg/mL(33.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 82 mg/mL (183.6 mM)

References and Literature

1. Timothy Perera, et al. Cancer Res. 2014, 74(19 Suppl):Abstract nr 1738. 2. Verstraete M, et al. BMC Cancer. 2015, 15:946.

Citations

1. Tao Z, Cui Y, Xu X, et al. FGFR redundancy limits the efficacy of FGFR4-selective inhibitors in hepatocellular carcinoma. Proceedings of the National Academy of Sciences. 2022, 119(40): e2208844119.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library FDA-Approved Kinase Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Approved Drug Library

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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 μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Erdafitinib 1346242-81-6 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors FGFR inhibit Fibroblast growth factor receptor JNJ42756493 Inhibitor JNJ-42756493 JNJ 42756493 inhibitor

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