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Fisogatinib

Name: Fisogatinib
Brand: TargetMol
SKU: T3456
Price: 48 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3456Cas No. 1707289-21-1

Alias BLU-554, BLU554, BLU 554

Fisogatinib (BLU-554) is a highly potent, selective and orally active FGFR4 inhibitor with an IC50 value of 5 nM and significant anti-tumor activity in hepatocellular carcinoma models dependent on FGFR4 signaling.

Fisogatinib

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Purity: 99.87%

Catalog No. T3456Alias BLU-554, BLU554, BLU 554Cas No. 1707289-21-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
5 mg	$123	In Stock	In Stock
10 mg	$186	In Stock	In Stock
25 mg	$327	In Stock	In Stock
50 mg	$493	In Stock	In Stock
100 mg	$745	In Stock	In Stock
500 mg	$1,490	-	In Stock
1 mL x 10 mM (in DMSO)	$136	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.87%

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Fisogatinib (BLU-554) is a highly potent, selective and orally active FGFR4 inhibitor with an IC50 value of 5 nM and significant anti-tumor activity in hepatocellular carcinoma models dependent on FGFR4 signaling.
Targets&IC50	FGFR4:5 nM
In vitro	METHODS: Transepithelial drug transport was assessed using polarized monolayers of MDCK-II parental cells and their subclones overexpressing hABCB1, hABCG2, or mAbcg2 treated with Fisogatinib (BLU-554) (5 μM). RESULTS Fisogatinib (BLU-554) was moderately transported by hABCB1 and slightly transported by mAbcg2. [4]
In vivo	METHODS: A preliminary experiment was conducted in which male wild-type and Oatp1a/1b−/− mice were given Fisogatinib (BLU-554) (10 mg/kg, oral) and the plasma concentration before 4 hours and the liver-to-plasma ratio at 4 hours were analyzed. RESULTS Oatp1a/1b protein had little effect on the oral efficacy or liver distribution of Fisogatinib (BLU-554) in mice. [4]
Kinase Assay	The Ki value and mode of inhibition of LY2801653 for the MET kinase activity are determined using a radiometric filter-binding assay. Reactions are carried out in 96-well plates in Enzyme dilution buffer (EDB) compose of 50 mM Tris HCl pH 7.5, 2 mM DTT, 0.005% Triton X-100, 10 mM MgCl2, and 250 ?M EDTA. Serially diluted LY2801653 (final concentration 250 to 0 nM) are followed by the addition of a series of 8 concentrations of 33P-γ-ATP (final concentration 400 to 10 μM ATP), and 5 nM enzyme (final concentration). After a 2-hour incubation, PolyGluTyr synthetic protein substrate (final 150 μg/mL) is added to initiate the 30-minute kinase reaction. Reactions are quenched with 10% H3PO4, transfer to a pre-wetted Multiscreen anionic phosphocellulose 96-well filter plate, and washed; radioactivity is measured with a scintillation counter. The experimental data are fit to a global mix model inhibition equation using GraphPad Prism softwar to generate an alpha value to determine the modality of inhibition and to calculate the Ki value for LY2801653[1].
Synonyms	BLU-554, BLU554, BLU 554

Chemical Properties

Molecular Weight	503.38
Formula	C₂₄H₂₄Cl₂N₄O₄
Cas No.	1707289-21-1
Smiles	COc1cc(OC)c(Cl)c(c1Cl)-c1ccc2nc(N[C@@H]3COCC[C@@H]3NC(=O)C=C)ncc2c1
Relative Density.	1.39 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 2 mg/mL (3.97 mM), Sonication is recommended.

DMSO: 250 mg/mL (496.64 mM), Sonication is recommended.

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

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.56 mM), Sonication is recommended.

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

	1mg	5mg	10mg	50mg
1 mM	1.9866 mL	9.9329 mL	19.8657 mL	99.3285 mL

DMSO

	1mg	5mg	10mg	50mg
5 mM	0.3973 mL	1.9866 mL	3.9731 mL	19.8657 mL
10 mM	0.1987 mL	0.9933 mL	1.9866 mL	9.9329 mL
20 mM	0.0993 mL	0.4966 mL	0.9933 mL	4.9664 mL
50 mM	0.0397 mL	0.1987 mL	0.3973 mL	1.9866 mL
100 mM	0.0199 mL	0.0993 mL	0.1987 mL	0.9933 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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