Futibatinib

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].

Product Specifications

CAS Number

[1448169-71-8]

Product Name Alternative

TAS-120

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

FGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/FGFR-IN-1.html

Purity

99.90

Solubility

DMSO : ≥ 29 mg/mL

Smiles

O=C(C=C)N(C1)CC[C@@H]1N(N=C2C#CC3=CC(OC)=CC(OC)=C3)C4=C2C(N)=NC=N4

Molecular Formula

C22H22N6O3

Molecular Weight

418.45

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.|[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.