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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $48 | In Stock | In Stock | |
| 5 mg | $123 | In Stock | In Stock | |
| 10 mg | $179 | In Stock | In Stock | |
| 25 mg | $347 | In Stock | In Stock | |
| 50 mg | $538 | In Stock | In Stock | |
| 100 mg | $697 | - | In Stock | |
| 200 mg | $989 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $136 | In Stock | In Stock |
| 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] |
| Synonyms | TAS120, FGFR-IN-1 |
| Molecular Weight | 418.45 |
| Formula | C22H22N6O3 |
| Cas No. | 1448169-71-8 |
| Smiles | COc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12 |
| Relative Density. | 1.33 g/cm3 (Predicted) |
| 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: 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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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