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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

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Purity: 99.36%
Catalog No. T3726Alias JNJ-42756493Cas No. 1346242-81-6
Erdafitinib (JNJ-42756493), a quinoxaline derivative, targets FGFR1/2/3/4.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$39In StockIn Stock
10 mg$64In StockIn Stock
25 mg$97In StockIn Stock
50 mg$155In StockIn Stock
100 mg$238In StockIn Stock
500 mg$588-In Stock
1 mL x 10 mM (in DMSO)$43In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.36%
Color:Yellow
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Product Introduction

Bioactivity
Description
Erdafitinib (JNJ-42756493), a quinoxaline derivative, targets 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)
SynonymsJNJ-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
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 15 mg/mL (33.59 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 32 mg/mL (71.66 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8.2 mg/mL (18.36 mM), Solution.
Please add the 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. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.2394 mL11.1972 mL22.3944 mL111.9721 mL
5 mM0.4479 mL2.2394 mL4.4789 mL22.3944 mL
10 mM0.2239 mL1.1197 mL2.2394 mL11.1972 mL
20 mM0.1120 mL0.5599 mL1.1197 mL5.5986 mL
DMSO
1mg5mg10mg50mg
50 mM0.0448 mL0.2239 mL0.4479 mL2.2394 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Dose Conversion

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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

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