Cat. No.: HY-100818

Futibatinib

(Synonyms: TAS-120)

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC₅₀s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC₅₀s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM).

For research use only. We do not sell to patients.

Purity: 99.90%
CAS No.: 1448169-71-8
Formula: C₂₂H₂₂N₆O₃
Molecular Weight:418.45

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Futibatinib Chemical Structure

CAS No.: 1448169-71-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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)

Cellular Effect

Cell Line	Type	Value	Description	References
Huh-7	IC₅₀	>10 μM Compound: TAS-120	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
NCI-H1581	IC₅₀	0.007 μM Compound: TAS-120	Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
NCI-H460	IC₅₀	>10 μM Compound: TAS-120	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
RT-112	IC₅₀	19.6 nM Compound: Futibatinib	Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	390 nM Compound: Futibatinib	Antiproliferative activity against human RT-112 cells expressing FGFR3 V555M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 V555M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	6.7 nM Compound: Futibatinib	Antiproliferative activity against human RT-112 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	73.4 nM Compound: Futibatinib	Antiproliferative activity against human RT-112 cells expressing FGFR3 N540K mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 N540K mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	74.3 nM Compound: Futibatinib	Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
SK-HEP1	IC₅₀	0.152 μM Compound: TAS-120	Antiproliferative activity against human SK-HEP1 cells expressing FGFR4 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human SK-HEP1 cells expressing FGFR4 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
SNU1	IC₅₀	>5000 nM Compound: 5; TAS-120	Cytotoxicity against human SNU1 cells assessed as inhibition of cell growth measured after 72 hrs by cell titer glo assay Cytotoxicity against human SNU1 cells assessed as inhibition of cell growth measured after 72 hrs by cell titer glo assay	[PMID: 37077386]
SNU-16	IC₅₀	0.004 μM Compound: TAS-120	Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
SNU-16	IC₅₀	3.7 nM Compound: 5; TAS-120	Cytotoxicity against human SNU-16 cells assessed as inhibition of cell growth measured after 72 hrs by cell titer glo assay Cytotoxicity against human SNU-16 cells assessed as inhibition of cell growth measured after 72 hrs by cell titer glo assay	[PMID: 37077386]
SNU-16	IC₅₀	4.7 nM Compound: Futibatinib	Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]

In Vitro

Futibatinib (TAS-120) covalently binds to a highly conserved P-loop cysteine residue in the ATP pocket of FGFR^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Futibatinib (TAS-120) (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor effect in mice. Futibatinib (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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1448169-71-8
Appearance Solid
Molecular Weight 418.45
Formula C₂₂H₂₂N₆O₃
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
Synonyms

TAS-120
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (8)

All WBBio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

Cell

A 3D morphogenetic blueprint for metastatic outgrowth in breast cancer. [Abstract]

2026 Mar 31:S0092-8674(26)00276-X. PMID: 41923644
Cancer Res

C-terminal Truncation and Fusion Partner Determine Oncogenicity of FGFR3. [Abstract]

2025 Dec 29. PMID: 41460723
Proc Natl Acad Sci U S A

Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2. [Abstract]

2024 Feb 6;121(6):e2317756121. PMID: 38300868

Futibatinib purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Feb 6;121(6):e2317756121. [Abstract]

Dose-dependent inhibition of FGFR2 in the FGFR2-amplified SNU-16 gastric cancer xenograft model. Female BALB/c mice were given twice daily oral doses of 1, 5, or 10 mg/kg Lirafugratinib. Lirafugratinib was compared with clinically relevant doses of Futibatinib (2 mg/kg, TID, oral) and Pemigatinib. Tumor tissue was collected at a designated time point on day four after the last dose. Tumor lysates were analyzed by HTRF analysis of pFGFR2 (Y653/654) and total FGFR2 (tFGFR2).

Futibatinib purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Feb 6;121(6):e2317756121. [Abstract]

Lirafugratinib spares FGFR1-driven hyperphosphatemia in vivo. Following 14 d of dosing Futibatinib (3 mg/kg, BID; 10 mg/kg, QD; oral) and Lirafugratinib to Sprague Dawley rats at the indicated doses and schedules, blood was collected from all animals for serum phosphate analysis (n = 5/group).
Dev Cell

Vagal sensory neuron-derived FGF3 controls insulin secretion. [Abstract]

2025 Jan 6;60(1):51-61.e4. PMID: 39413782
J Pharm Biomed Anal

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. [Abstract]

2026 Feb 15:269:117253. PMID: 41241972

Futibatinib purchased from MedChemExpress. Usage Cited in: J Pharm Biomed Anal. 2026 Feb 15:269:117253. [Abstract]

Representative SRM chromatograms of blank liver microsomes and a 60-min microsomal incubation sample. Gunagratinib (RT = 1.18 min) was monitored at m/z 424.2→407.3, and Futibatinib (IS; RT = 0.88 min) at m/z 419.2→296.1.
J Pharm Biomed Anal

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. [Abstract]

2022 May 30;214:114731. PMID: 35325798

Futibatinib purchased from MedChemExpress. Usage Cited in: J Pharm Biomed Anal. 2022 May 30;214:114731. [Abstract]

QC samples were stored at room temperature (~24 ℃) for 0, 1, 2 and 4 hours before analysis to assess the stability of the Futibatinib (0.02-2 μM).

Futibatinib purchased from MedChemExpress. Usage Cited in: J Pharm Biomed Anal. 2022 May 30;214:114731. [Abstract]

QC samples were stored at autosampler temperature (4 ℃) for 0, 6, 12, and 24 hours prior to analysis to assess the stability of the Futibatinib (0.02-2 μM).
bioRxiv

2025 Nov 18.
University of Auckland

2025.

Solvent & 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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3898 mL

11.9489 mL

23.8977 mL

5 mM

0.4780 mL

2.3898 mL

4.7795 mL

10 mM

0.2390 mL

1.1949 mL

2.3898 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (4.97 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.97 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Animal Administration^[1]

It is transplanted to the right chest of the anti-tumor effect human gastric cancer strain (OCUM-2MD3) the old 6-week-old male nude rats with intermittent administration schedule in Test Example 7 rat. Measuring the major axis of tumor (mm) and minor axis (mm) after tumor implantation, the tumor volume: After calculating the (tumor volume TV), allocates the mouse average TV each group to be equal in each group, the the days that are conducted grouped the (n=5) is the day 0. Futibatinib (TAS-120) 3 mg/kg/day, 30 mg/kg/day, is prepared so as to 100 mg/kg/day, 3 mg/kg/day is daily administered orally, 30 mg/kg/day is administered orally every other day, 100 mg/kg/day is performed oral administration of 2 time/week from day 1, provided with the evaluation period of 14 days, the final valuation date it is day 15.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Goyal L, et al. TAS-120 Overcomes Resistance to ATP-Competitive FGFR Inhibitors in Patients with FGFR2 Fusion-Positive Intrahepatic Cholangiocarcinoma. Cancer Discov. 2019 Aug;9(8):1064-1079. [Content Brief]

[2]. Kalyukina M, et al. TAS-120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure. ChemMedChem. 2019 Feb 19;14(4):494-500. [Content Brief]

[3]. Lamarca A, et al. Molecular targeted therapies: Ready for "prime time" in biliary tract cancer [published online ahead of print, 2020 Mar 12]. J Hepatol. 2020;S0168-8278(20)30165-3. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3898 mL	11.9489 mL	23.8977 mL	59.7443 mL
	5 mM	0.4780 mL	2.3898 mL	4.7795 mL	11.9489 mL
	10 mM	0.2390 mL	1.1949 mL	2.3898 mL	5.9744 mL
	15 mM	0.1593 mL	0.7966 mL	1.5932 mL	3.9830 mL
	20 mM	0.1195 mL	0.5974 mL	1.1949 mL	2.9872 mL
	25 mM	0.0956 mL	0.4780 mL	0.9559 mL	2.3898 mL
	30 mM	0.0797 mL	0.3983 mL	0.7966 mL	1.9915 mL
	40 mM	0.0597 mL	0.2987 mL	0.5974 mL	1.4936 mL
	50 mM	0.0478 mL	0.2390 mL	0.4780 mL	1.1949 mL
	60 mM	0.0398 mL	0.1991 mL	0.3983 mL	0.9957 mL

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Futibatinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

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Publications Citing Use of MedChemExpress (MCE) Futibatinib

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Futibatinib Related Classifications

HY-100818 Related Classifications