Futibatinib

SKU: orb1302144

Description

Futibatinib (TAS-120) is a highly selective, irreversible, and orally bioavailable inhibitor of FGFR1-4. It demonstrates potent activity in preclinical models of FGFR-dysregulated cancers, supporting its investigation in both in vitro and in vivo research for oncology and targeted therapy applications.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1448169-71-8
• MW: 418.45
• Purity: 99.44% (May vary between batches)
• Formula: C₂₂H₂₂N₆O₃
• SMILES: COc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12
• Target: FGFR
• Solubility: DMSO:62.5 mg/mL (149.36 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (5.97 mM)

Bioactivity

• Target IC50:
  FGFR2:1.3 nM (IC50)|FGFR3:1.6 nM (IC50)|FGFR2 (E566G):2.4 nM (IC50)|FGFR2 (N550H):3.6 nM (IC50)|FGFR4:8.3 nM (IC50)|FGFR2 (V5651):1-3 nM (IC50)|FGFR1:3.9 nM (IC50)|FGFR2 (WT):0.3 nM (IC50)
• In Vivo:
  METHODS: Patient-derived ICC xenograft (PDX) model mice were treated with 25 mg/kg Futibatinib（TAS-120） orally daily for 3 and 14 days prior to harvest. Tumor samples were collected for biochemical analysis and histological processing. RESULTS Treatment of MG69 PDX tumors with TAS-120 (beginning when they reached ~500 mm in volume 3) resulted in tumor regression and complete proliferation arrest, with effects evident within three days and sustained over the 14-day treatment course.
• In Vitro:
  TAS-120 (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor effect in mice. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TAS120, TAS-120, TAS 120, Fibroblast growth factor receptor, FGFR-IN-1, FGFR, Futibatinib, Inhibitor, inhibit

Compound Identifiers

PubChem CID

71621331