| Field | Specification |
|---|---|
| Target | |
| Alternative names | TAS-120 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H22N6O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Futibatinib, also known as TAS-120, is an orally bioavailable, highly selective, irreversible FGFR inhibitor, with IC50 values of 3.9 nM, 1.3 nM, 1.6 nM and 8.3 nM for FGFR1-4, respectively. It inhibits mutant and wild-type FGFR2 with similar potency (wild-type FGFR2 = 0.9 nM; V5651 = 1-3 nM; N550H = 3.6 nM; E566G = 2.4 nM)[1][2][3]. It is supplied as a white to yellow solid (C22H22N6O3, MW 418.45) at 99.90% purity.
Physical & Chemical Properties
| CAS Number | 1448169-71-8 |
|---|---|
| Molecular Formula | C22H22N6O3 |
| Molecular Weight | 418.45 g/mol |
| Purity | 99.90% |
| Appearance | Solid |
| Color | White to yellow |
| SMILES | O=C(C=C)N(C1)CC[C@@H]1N(N=C2C#CC3=CC(OC)=CC(OC)=C3)C4=C2C(N)=NC=N4 |
| Target | FGFR1, FGFR2, FGFR3, FGFR4, Wild-type FGFR2, FGFR2 V5651, FGFR2 N550H, FGFR2 E566G |
| Signaling Pathway | Protein Tyrosine Kinase/RTK |
| Solubility | In Vitro: DMSO: ≥ 29 mg/mL (69.30 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 1 year; -20°C, 6 months. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[3]
|
FGFR1 3.9 nM (IC50) |
FGFR2 1.3 nM (IC50) |
FGFR3 1.6 nM (IC50) |
FGFR4 8.3 nM (IC50) |
wild-type FGFR2 0.3 nM (IC50) |
FGFR2 V5651 1-3 nM (IC50) |
FGFR2 N550H 3.6 nM (IC50) |
FGFR2 E566G 2.4 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 29 mg/mL (69.30 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 1 year) or -20°C (up to 6 months); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 2.08 mg/mL (4.97 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.08 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.08 mg/mL (4.97 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.08 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.08 mg/mL (4.97 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Futibatinib (TAS-120) binds covalently to a highly conserved P-loop cysteine residue located in the ATP pocket of FGFR[1].
In Vivo
In mice, Futibatinib (TAS-120) at 3, 30, 100 mg/kg/day (p.o.) exerts an anti-tumor effect. Intermittent dosing of Futibatinib (TAS-120) at moderate intervals, such as every other day and 2 times/week, also shows an anti-tumor effect, reduces the sustained elevation of blood phosphorus level and weight suppression, and gives antitumor effectiveness as with daily administration[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Animal Administration[1]
Transplant human gastric cancer strain (OCUM-2MD3) into the right chest of 6-week-old male nude rats for the anti-tumor effect test with the intermittent administration schedule of Test Example 7. After tumor implantation, measure the major axis (mm) and minor axis (mm) of the tumor and calculate the tumor volume (TV). Allocate the mice to groups (n=5) so that the average TV is equal in each group; the day of grouping is day 0. Prepare Futibatinib (TAS-120) at 3 mg/kg/day, 30 mg/kg/day, and 100 mg/kg/day. Administer 3 mg/kg/day orally every day, 30 mg/kg/day orally every other day, and 100 mg/kg/day orally 2 time/week from day 1. Set the evaluation period at 14 days, with the final evaluation date on day 15.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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A 3D morphogenetic blueprint for metastatic outgrowth in breast cancer. Cell 2026 Jun 11;189(12):3701-3718.e30. PMID: 41923644
C-terminal Truncation and Fusion Partner Determine Oncogenicity of FGFR3. Cancer Res 2025 Dec 29. PMID: 41460723
Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2. Proc Natl Acad Sci U S A 2024 Feb 6;121(6):e2317756121. PMID: 38300868
Vagal sensory neuron-derived FGF3 controls insulin secretion. Dev Cell 2025 Jan 6;60(1):51-61.e4. PMID: 39413782
FGFR2 fusion-driven cholangiocarcinoma is characterized by a distinct neutrophil-enriched tumor microenvironment in a syngeneic murine model. JHEP Rep 2026 Jul 21:101964. PMID: 42480814
Metabolic stability assessment and metabolite profiling of gunagratinib, a novel FGFR inhibitor, in rat, monkey and human liver microsomes by an integrated analysis method based on HPLC-MS/MS and HPLC-Orbitrap-HRMS. J Pharm Biomed Anal 2026 Feb 15:269:117253. PMID: 41241972
Quantification of the irreversible fibroblast growth factor receptor inhibitor futibatinib by UPLC-MS/MS: Application to the metabolic stability assay in human liver microsomes for the estimation of its in vitro hepatic intrinsic clearance. J Pharm Biomed Anal 2022 May 30;214:114731. PMID: 35325798
bioRxiv. 2025 Nov 18.
University of Auckland. 2025.
