Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Futibatinib [1448169-71-8]

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Referência HY-100818-5mg

Tamanho : 5mg

Marca : MedChemExpress

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Description

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)^[1]^[2]^[3].

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.

Solvant et solubilité

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.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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.

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.

Pureté et documentation

Purity: 99.90%

Fiche technique (281 KB) SDS (396 KB)

COA (252 KB) HNMR (300 KB) RP-HPLC (258 KB) MS (71 KB)

Instruction de manipulation (2659 KB)

Références

[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]

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Referência HY-100818-5mg

Marca : MedChemExpress

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