Home Protein Tyrosine Kinase FGFR inhibitor Futibatinib (TAS-120) For research use only.

Futibatinib (TAS-120)

Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

Futibatinib (TAS-120) Chemical Structure

Futibatinib (TAS-120) Chemical Structure

CAS No. 1448169-71-8

Purity & Quality Control

Futibatinib (TAS-120) Related Products

Signaling Pathway

FGFR Signaling Pathways

FGFR Signaling Pathway

Biological Activity

Description Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
Targets
FGFR2 [1]
(Cell-free assay)		 FGFR3 [1]
(Cell-free assay)		 FGFR1 [1]
(Cell-free assay)		 FGFR4 [1]
(Cell-free assay)
1.4 nM 1.6 nM 1.8 nM 3.7 nM
In vitro
In vitro

Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05827614 Recruiting
Non-small Cell Lung Cancer|Non-Small Cell Lung Adenocarcinoma|Non-Small Cell Squamous Lung Cancer|Head and Neck Squamous Cell Carcinoma|Esophageal Cancer|Gastric Cancer|Breast Cancer|Bladder Cancer|Ovarian Cancer|Endometrial Cancer|Liposarcoma
Boundless Bio
 March 24 2023 Phase 1
NCT04965818 Terminated
Advanced or Metastatic Solid Tumors Irrespective of Gene Alterations|Non-Small Cell Lung Cancer|KRAS Gene Mutation
Taiho Oncology Inc.
 September 20 2021 Phase 1
NCT05036681 Recruiting
Metastatic Cancer|Endometrium Cancer|Endometrial Carcinoma
M.D. Anderson Cancer Center|National Comprehensive Cancer Network
 September 30 2021 Phase 2
NCT04024436 Active not recruiting
Metastatic Breast Cancer|FGFR 1 High Amplification|FGFR2 Amplification
Taiho Oncology Inc.
 August 30 2019 Phase 2
NCT02052778 Completed
Cholangiocarcinoma|Urothelial Cancer|Advanced and Metastatic Cancer Patients With Tumors Harboring FGF/FGFR Tumors|Primary CNS Tumors|Breast Cancer|Gastric Cancer
Taiho Oncology Inc.
 July 21 2014 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 418.45 Formula

C22H22N6O3
CAS No. 1448169-71-8 SDF --
Smiles COC1=CC(=CC(=C1)C#CC2=NN(C3=NC=NC(=C23)N)C4CCN(C4)C(=O)C=C)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 84 mg/mL ( (200.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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