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Futibatinib

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Catalog No. T5044Cas No. 1448169-71-8
Alias TAS120, FGFR-IN-1

Futibatinib (TAS-120) is an orally active, potent, selective, highly bioavailable, and irreversible FGFR inhibitor with IC50 values ​​of 3.9, 1.3, 1.6, and 8.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. [2]

Futibatinib

Futibatinib

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Purity: 99.44%
Catalog No. T5044Alias TAS120, FGFR-IN-1Cas No. 1448169-71-8
Futibatinib (TAS-120) is an orally active, potent, selective, highly bioavailable, and irreversible FGFR inhibitor with IC50 values ​​of 3.9, 1.3, 1.6, and 8.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. [2]
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$48In StockIn Stock
5 mg$123In StockIn Stock
10 mg$179In StockIn Stock
25 mg$347In StockIn Stock
50 mg$538In StockIn Stock
100 mg$697-In Stock
200 mg$989-In Stock
1 mL x 10 mM (in DMSO)$136In 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:99.44%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Futibatinib (TAS-120) is an orally active, potent, selective, highly bioavailable, and irreversible FGFR inhibitor with IC50 values ​​of 3.9, 1.3, 1.6, and 8.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. [2]
Targets&IC50
FGFR2:1.3 nM (IC50), FGFR1:3.9 nM (IC50), FGFR2 (V5651):1-3 nM (IC50), FGFR2 (WT):0.3 nM (IC50), FGFR3:1.6 nM (IC50), FGFR4:8.3 nM (IC50), FGFR2 (N550H):3.6 nM (IC50), FGFR2 (E566G):2.4 nM (IC50)
In vitro
TAS-120 (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor effect in mice. TAS-120 shows anti-tumor effect by administering at moderate intervals, such as intermittent administration of every other day dosing and 2 times/week, and reducing the sustained elevation and weight suppression blood phosphorus level, and take a antitumor effective as daily administration.
In vivo
METHODS: Patient-derived ICC xenograft (PDX) model mice were treated with 25 mg/kg Futibatinib(TAS-120) orally daily for 3 and 14 days prior to harvest. Tumor samples were collected for biochemical analysis and histological processing.
RESULTS Treatment of MG69 PDX tumors with TAS-120 (beginning when they reached ~500 mm in volume 3) resulted in tumor regression and complete proliferation arrest, with effects evident within three days and sustained over the 14-day treatment course. [1]
SynonymsTAS120, FGFR-IN-1
Chemical Properties
Molecular Weight418.45
FormulaC22H22N6O3
Cas No.1448169-71-8
SmilesCOc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12
Relative Density.1.33 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 62.5 mg/mL (149.36 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 2.5 mg/mL (5.97 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
1mg5mg10mg50mg
1 mM2.3898 mL11.9489 mL23.8977 mL119.4886 mL
5 mM0.4780 mL2.3898 mL4.7795 mL23.8977 mL
10 mM0.2390 mL1.1949 mL2.3898 mL11.9489 mL
20 mM0.1195 mL0.5974 mL1.1949 mL5.9744 mL
50 mM0.0478 mL0.2390 mL0.4780 mL2.3898 mL
100 mM0.0239 mL0.1195 mL0.2390 mL1.1949 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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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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