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Futibatinib

MCE China：Futibatinib

Brand：MedChemExpress (MCE)

Cat. No.HY-100818

CAS：1448169-71-8

Synonyms：TAS-120

Purity：99.65%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months

Shipping：Room temperature in continental US; may vary elsewhere.

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).

In Vitro：Futibatinib (TAS-120) covalently binds to a highly conserved P-loop cysteine residue in the ATP pocket of FGFR[1].

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[1].

Animal Administration：It is transplanted to the right chest of the anti-tumor effect human gastric cancer strain (OCUM-2MD3) the old 6-week-old male nude rats with intermittent administration schedule in Test Example 7 rat. Measuring the major axis of tumor (mm) and minor axis (mm) after tumor implantation, the tumor volume: After calculating the (tumor volume TV), allocates the mouse average TV each group to be equal in each group, the the days that are conducted grouped the (n=5) is the day 0. Futibatinib (TAS-120) 3 mg/kg/day, 30 mg/kg/day, is prepared so as to 100 mg/kg/day, 3 mg/kg/day is daily administered orally, 30 mg/kg/day is administered orally every other day, 100 mg/kg/day is performed oral administration of 2 time/week from day 1, provided with the evaluation period of 14 days, the final valuation date it is day 15.

IC50 & Target：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)

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References：

[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]