Futibatinib (TAS-120)

Alias: Futibatinib; TAS-120; TAS 120; TAS120

Cat No.:V4847 Purity: ≥98%

COA Product Data Instructions for use SDS

Futibatinib (TAS-120) Chemical Structure CAS No.: 1448169-71-8
Product category: FGFR

This product is for research use only, not for human use. We do not sell to patients.

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Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Futibatinib (formerly also known as TAS 120; TAS-120) is a novel, potent, irreversible and orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential anticancer activity. Its IC50 values for inhibiting FGFR 1-4 are 3.9, 1.3, 1.6, and 8.3 nM, in that order. TAS-120 specifically and irreversibly binds to FGFR, inhibiting it. This may lead to increased cell death in tumor cells overexpressing FGFR, as well as the inhibition of the FGFR-mediated signal transduction pathway and tumor cell proliferation. Many different types of tumor cells express FGFR, a receptor tyrosine kinase that is critical to the growth, differentiation, and survival of tumor cells.

Biological Activity I Assay Protocols (From Reference)

Targets

FGFR1 (IC50 = 3.9 nM); FGFR2 (IC50 = 1.3 nM); FGFR3 (IC50 = 1.6 nM); FGFR4 (IC50 = 8.3 nM); wild-type FGFR2 (IC50 = 0.3 nM); FGFR2 V5651 (IC50 = 1-3 nM); FGFR2 N550H (IC50 = 3.6 nM); FGFR2 E566G (IC50 = 2.4 nM)

ln Vitro

Futibatinib (TAS-120) is a permanent fibroblast growth factor receptor (FGFR) inhibitor that inhibits all four FGFR subtypes, with enzyme half-lives (IC50) for FGFR1, FGFR2, FGFR3, and FGFR4 being 1.8 nM, 1.4 nM, 1.6 nM, and 3.7 nM, respectively.

ln Vivo

TAS-120 (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor effect in mice. By lowering the blood phosphorus level's sustained elevation and weight suppression, as well as by intermittently administering the drug every other day and twice a week, TAS-120 exhibits anti-tumor effects. Its daily administration is also effective.

Cell Assay

Overexpressing FGFR in a human gastric cancer cell line The Dulbecco's Modified Eagle (OCUM-2MD3) cells, which contain 10% fetal bovine serum (FBS) in medium (DMEM), are routinely passaged at a cell density of no more than 80%. In order to test the cytostatic activity, 3,000 cells per well are seeded in each well of 96-well flat-bottom plates. The cells are then suspended in the DMEM medium above and cultured for one day at 37°C in an incubator with 5% carbon dioxide gas. It is stage-diluted to 100 times the final concentration of the test compound in DMSO the following day. The test compound is diluted with DMSO solution and added to a final concentration of DMSO in each well of a culture plate containing cells at a rate of 0.5%, 5% carbon dioxide gas incubator, and then cultured for 72 hours at 37°C. Following the suggested protocols provided by Dojindo Laboratories, the number of cells is measured using a cell counting kit-8 72 hours after the test compound is added to the culture. The reagent kit is added to each plate, and the color reaction is carried out for a predetermined amount of time at 37°C in an incubator with 5% carbonic acid gas. A microplate reader is used to measure the absorbance at 450 nm after the reaction is finished. GI50 (nM) is the concentration of the test compound at which 50% inhibition occurs, which is calculated by applying the growth inhibition rate formula.

Animal Protocol

The old 6-week-old male nude rats with an intermittent administration schedule are transplanted to the right chest of the anti-tumor effect human gastric cancer strain (OCUM-2MD3). Measuring the tumor's volume after implantation and its major and minor axes in millimeters: The day 0 of the days that are conducted in groups of (n=5) is determined by allocating the mouse average TV to each group after the tumor volume TV has been calculated. Futibatinib (TAS-120) is prepared so that it contains 3 mg/kg/day and 30 mg/kg/day. 3 mg/kg/day is taken orally every day, while 30 mg/kg/day is taken orally every other day. 100 mg/kg/day is taken orally twice a week starting on day 1, with a 14-day evaluation period and a 15-day final valuation date.

References

[1]. 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.

[2]. 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.

[3]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C22H22N6O3
Molecular Weight	418.4485
Exact Mass	418.18
Elemental Analysis	C, 63.15; H, 5.30; N, 20.08; O, 11.47
CAS #	1448169-71-8
Appearance	Off-white to light beige solid powder
SMILES	COC1=CC(=CC(=C1)C#CC2=NN(C3=NC=NC(=C23)N)[C@H]4CCN(C4)C(=O)C=C)OC
InChi Key	KEIPNCCJPRMIAX-HNNXBMFYSA-N
InChi Code	InChI=1S/C22H22N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h4,9-11,13,15H,1,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1
Chemical Name	1-[(3S)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]pyrazolo[3,4-d]pyrimidin-1-yl]pyrrolidin-1-yl]prop-2-en-1-one
Synonyms	Futibatinib; TAS-120; TAS 120; TAS120
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)	DMSO: ≥ 29 mg/mL (~69.3 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 2.08 mg/mL (4.97 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.97 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More Solubility in Formulation 3: ≥ 2.08 mg/mL (4.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO: ≥ 29 mg/mL (~69.3 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 2.08 mg/mL (4.97 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: 2.08 mg/mL (4.97 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

View More

Solubility in Formulation 3: ≥ 2.08 mg/mL (4.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

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Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04189445	Active Recruiting	Drug: Futibatinib	Advanced or Metastatic Solid Tumor Myeloid or Lymphoid Neoplasms (MLN)	Taiho Oncology, Inc.	August 24, 2020	Phase 2
NCT04093362	Active Recruiting	Drug: TAS-120 Drug: Cisplatin/Gemcitabine	Advanced Cholangiocarcinoma FGFR2 Gene Rearrangements	Taiho Oncology, Inc.	March 1, 2020	Phase 3
NCT04024436	Active Recruiting	Drug: Futibatinib Drug: Futibatinib plus Fulvestrant	Metastatic Breast Cancer FGFR 1 High Amplification Metastatic Melanoma	Taiho Oncology, Inc.	August 30, 2019	Phase 2
NCT02052778	Active Recruiting	Drug: Futibatinib	Urothelial Cancer Primary CNS Tumors	Taiho Oncology, Inc.	July 2014	Phase 1 Phase 2
NCT05615818	Not yet recruiting	Drug: Futibatinib Drug: Ivosidenib	Biliary Tract Neoplasms	UNICANCER	January 2024	Phase 3

Biological Data

TAS-120 is clinically effective in FGFR2 fusion-positive ICC patients whose tumors acquired resistance to BGJ398 or Debio1347. Cancer Discov . 2019 Aug;9(8):1064-1079.
Structural modeling of secondary FGFR2 kinase domain mutations with TAS-120. Cancer Discov . 2019 Aug;9(8):1064-1079.