Futibatinib

• CAT Number: I001727
• CAS Number: 1448169-71-8
• Molecular Formula: C22H22N6O3
• Molecular Weight: 418.45
• Purity: 98%
• Synonyms: 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
• Target: FGFR
• Target Protein: P11362,P21802,P22607,P22455
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IC50: FGFR1:3.9 nM (IC50)
• InChI: 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
• InChIKey: KEIPNCCJPRMIAX-HNNXBMFYSA-N
• SMILES: COC1=CC(=CC(=C1)C#CC2=NN(C3=NC=NC(=C23)N)[C@H]4CCN(C4)C(=O)C=C)OC

Futibatinib（Cat No.:I001727）is an oral, selective fibroblast growth factor receptor (FGFR) inhibitor used for the treatment of advanced cancers, particularly those with FGFR gene alterations, such as cholangiocarcinoma. By targeting and inhibiting FGFR1-4, Futibatinib blocks the aberrant signaling pathways that drive tumor growth and survival. It is especially effective in patients with FGFR2 fusions or mutations, offering a targeted therapy option where few treatments exist. With demonstrated efficacy in clinical trials and a manageable safety profile, Futibatinib represents a significant advancement for patients with FGFR-altered cancers.

Reference

[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]