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FGFR4-IN-5

Name: FGFR4-IN-5
Brand: TargetMol
SKU: T37425
Rating: 4.5 (1 reviews)

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Catalog No. T37425Cas No. 1628793-01-0

Alias FGFR4-IN-5

FGFR4-IN-5, a covalent FGFR4 inhibitor, demonstrates potency and selectivity with an IC50 value of 6.5 nM. Exhibiting significant in vivo anti-tumor activity, it is applicable for research in hepatocellular carcinoma [1].

FGFR4-IN-5

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Catalog No. T37425Alias FGFR4-IN-5Cas No. 1628793-01-0

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,670	6-8 weeks	6-8 weeks
50 mg	$2,180	6-8 weeks	6-8 weeks
100 mg	$2,800	6-8 weeks	6-8 weeks

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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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Product Introduction

Bioactivity

Description	FGFR4-IN-5, a covalent FGFR4 inhibitor, demonstrates potency and selectivity with an IC50 value of 6.5 nM. Exhibiting significant in vivo anti-tumor activity, it is applicable for research in hepatocellular carcinoma [1].
Targets&IC50	FGFR4:6.5 nM (IC50), FGFR2:505 nM (IC50)
In vivo	FGFR4-IN-5, administered via oral gavage at 10 mg/kg (single dose), shows high Cmax and low clearance, with Cmax values of 423 ng/ml in mice, 588 ng/ml in rats, and 2820 ng/ml in cynomolgus monkeys, and oral bioavailability of 20%, 12%, and 27%, respectively [1]. FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) demonstrates significant antitumor activity in an orthotopic Hep3B HTX model [1]. FGFR4-IN-5 (oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days) induces dose-dependent tumor growth inhibition, with regression at 30 and 100 mg/kg and %δT/δC values of 67% and 70%, respectively, while sorafenib (100 mg/kg; once daily) shows no in vivo benefit [1].
Synonyms	FGFR4-IN-5

Chemical Properties

Molecular Weight	520.37
Formula	C₂₃H₂₃Cl₂N₅O₅
Cas No.	1628793-01-0
Smiles	COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(N[C@@H]3COC[C@@H]3NC(=O)C=C)nc2n(C)c1=O

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (192.17 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.34 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9217 mL	9.6085 mL	19.2171 mL	96.0855 mL
5 mM	0.3843 mL	1.9217 mL	3.8434 mL	19.2171 mL
10 mM	0.1922 mL	0.9609 mL	1.9217 mL	9.6085 mL
20 mM	0.0961 mL	0.4804 mL	0.9609 mL	4.8043 mL
50 mM	0.0384 mL	0.1922 mL	0.3843 mL	1.9217 mL
100 mM	0.0192 mL	0.0961 mL	0.1922 mL	0.9609 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