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Erdafitinib

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Catalog No. T3726Cas No. 1346242-81-6
Alias JNJ-42756493

Erdafitinib (JNJ-42756493), a quinoxaline derivative, targets FGFR1/2/3/4.

Erdafitinib

Erdafitinib

🥰Excellent
Purity: 99.07%
Catalog No. T3726Alias JNJ-42756493Cas No. 1346242-81-6
Erdafitinib (JNJ-42756493), a quinoxaline derivative, targets FGFR1/2/3/4.
Pack SizePriceAvailabilityQuantity
5 mg$39In Stock
10 mg$64In Stock
25 mg$97In Stock
50 mg$155In Stock
100 mg$238In Stock
500 mg$588In Stock
1 mL x 10 mM (in DMSO)$43In Stock
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Purity:99.07%
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Product Introduction

Bioactivity
Description
Erdafitinib (JNJ-42756493), a quinoxaline derivative, targets FGFR1/2/3/4.
Targets&IC50
FGFR2:2.5nM, FGFR4:5.7 nM, FGFR3:3.0nM, FGFR1:1.2 nM
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)
AliasJNJ-42756493
Chemical Properties
Molecular Weight446.54
FormulaC25H30N6O2
Cas No.1346242-81-6
SmilesCOc1cc(OC)cc(c1)N(CCNC(C)C)c1ccc2ncc(nc2c1)-c1cnn(C)c1
Relative Density.1.20 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 15 mg/mL (33.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 5.63 mg/mL (12.6 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8.2 mg/mL (18.36 mM), In vivo: Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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