Futibatinib
Binding Mode- Product Name
- Futibatinib
- CAS No.
- 1448169-71-8
- Chemical Name
- Futibatinib
- Synonyms
- Futibatinib;1-[(3S)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidinyl]-2-propen-1-one;CS-2344;CS-2681;FGFR-IN-1;2H6]-Futibatinib;Futibatinib Crude;FUTIBATINIB;TAS120;TAS-120 (Futibatinib);Bexagliflozin Impurity 14
- CBNumber
- CB03155059
- Molecular Formula
- C22H22N6O3
- Formula Weight
- 418.45
- MOL File
- 1448169-71-8.mol
Futibatinib Property
- Boiling point:
- 733.8±60.0 °C(Predicted)
- Density
- 1.33±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:38.0(Max Conc. mg/mL);90.81(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);71.69(Max Conc. mM)
DMF:PBS (pH 7.2) (1:5):0.16(Max Conc. mg/mL);0.38(Max Conc. mM)
Ethanol:0.5(Max Conc. mg/mL);1.19(Max Conc. mM) - form
- A crystalline solid
- pka
- 3.60±0.30(Predicted)
- color
- White to yellow
- InChIKey
- KEIPNCCJPRMIAX-HNNXBMFYSA-N
- SMILES
- C(N1CC[C@H](N2C3C(C(C#CC4=CC(OC)=CC(OC)=C4)=N2)=C(N)N=CN=3)C1)(=O)C=C
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 21136
- Product name
- TAS 120
- Purity
- ≥98%
- Packaging
- 500μg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 21136
- Product name
- TAS 120
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $89
- Updated
- 2024/03/01
- Product number
- 21136
- Product name
- TAS 120
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $356
- Updated
- 2024/03/01
- Product number
- 21136
- Product name
- TAS 120
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $656
- Updated
- 2024/03/01
- Product number
- T773508
- Product name
- TAS-120
- Packaging
- 1mg
- Price
- $90
- Updated
- 2021/12/16
Futibatinib Chemical Properties,Usage,Production
Binding Mode
In the co-crystal structure with FGFR1,2,3 the
pyrazolopyrimidine core forms two hydrogen bonds
to the amide NH of Ala564 and amide oxygen of
Glu562 of the hinge region. The dimethoxyphenyl
ring, similarly to other FGFR1-selective inhibitors,
occupies a conserved hydrophobic pocket, forming
a single hydrogen bond to Asp641. Most importantly,
the inhibitor is irreversibly attached to the protein via
a covalent bond between the acrylamide group and
the reactive P-loop Cys488 (Figs. 1, 2).
Uses
Futibatinib is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. Futibatinib selectively and irreversibly binds to and inhibits FGFR, which may result in the inhibition of both the FGFR-mediated signal transduction pathway and tumor cell proliferation, and increased cell death in FGFR-overexpressing tumor cells. FGFR is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival and its expression is upregulated in many tumor cell types.
Application
Futibatinib has received accelerated approval in the U.S. for the treatment of patients with advanced solid tumors that carry FGFR gene mutations. In addition, it is approved in the U.S. for the treatment of patients with cholangiocarcinoma whose disease has progressed after prior chemotherapy. The development and approval of Futibatinib provides a new targeted treatment option for cancer patients that carry FGFR mutations, especially for those who are resistant or intolerant to existing treatment options.
brand name
Lytgobi
General Description
Class: receptor tyrosine kinase; Treatment: Cholangiocarcinoma; Other name: TAS 120; Elimination half-life = 2.9 h; Protein binding = 95%
Synthesis
The synthesis of Futibatinib is as follows:
2 methanesulfonate (25.0 g), water (69 mL), and acetonitrile (158 mL) were placed in a reaction vessel, and a 5N aqueous sodium hydroxide solution (35 mL) was added thereto. A solution prepared by diluting 3-chloropropionyl chloride (6.27 g) with acetonitrile (50 mL) was added over a period of 10 minutes. After completion of the dropwise addition, the mixture was stirred at 30° C. for 30 minutes. The reaction solution was partially taken out and measured by HPLC (condition 3). The peak area of compound B was confirmed to be less than 0.1% of the total peak area. At this stage, the diamide compound and the 3CP diamide compound were not detected in HPLC. Thereafter, a 5N aqueous sodium hydroxide solution (25 mL) was further added, and the mixture was stirred at 30° C. for 4 hours. The reaction solution was partially taken out and measured by HPLC (condition 3). The peak area of the A-1-3CP compound was confirmed to be less than 0.1% of the total peak area. After completion of the reaction, water (550 mL) was added over a period of 2 hours. After completion of the dropwise addition, the internal temperature was adjusted to 25° C., and the mixture was stirred for 1.5 hours. The insoluble matter was collected by filtration and washed with water (125 mL), followed by drying the washed matter at 60° C. under reduced pressure, thereby obtaining the Futibatinib (16.02 g, yield 85.3%).
in vitro
Futibatinib (TAS-120) covalently binds to a highly conserved P-loop cysteine residue in the ATP pocket of FGFR.
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.
target
Primary target: Pan-EGFR
Futibatinib Preparation Products And Raw materials
Raw materials
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View Lastest Price from Futibatinib manufacturers
- Product
- FGFR-IN-1 1448169-71-8
- Price
- US $0.01/KG
- Min. Order
- 1KG
- Purity
- 98%; 99%
- Supply Ability
- 500g;1kg； 25kg
- Release date
- 2020-01-09