BLU-554

SKU: orb1225954

Description

BLU-554 (Fisogatinib, BLU554) is a novel potent, highly selective and orally bioavailable inhibitor of FGFR4 designed for hepatocellular carcinoma (HCC) with FGFR4 pathway activation; targets FGFR4 while sparing other members of the FGFR family and showing little to no inhibition of all other kinases.Liver Cancer Phase 1 Clinical(In Vivo):Tissue distribution of Fisogatinib (10 mg/kg; oral gavage; for 4 hours; FVB/NRj mice) in wild-type mice is as follows; tissue concentrations decreases in the order liver > kidney > small intestine > spleen > brain. The high Fisogatinib liver-to-plasma ratio suggests there is a relatively high amount of the drug being transported into the liver.

Key Properties

• CAS Number: 1707289-21-1
• MW: 503.3777
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₄Cl₂N₄O₄
• SMILES: COC1=CC(=C(C(=C1Cl)C2=CC3=CN=C(N=C3C=C2)NC4COCCC4NC(=O)C=C)Cl)OC
• Target: FGFR
• Solubility: DMSO: ≥ 25 mg/mL

Bioactivity

• In Vivo:
  Tissue distribution of Fisogatinib (10 mg/kg; oral gavage; for 4 hours; FVB/NRj mice) in wild-type mice is as follows; tissue concentrations decreases in the order liver > kidney > small intestine > spleen > brain. The high Fisogatinib liver-to-plasma ratio suggests there is a relatively high amount of the drug being transported into the liver. Animal model: Wild type male mice(FVB/NRj, 11-14 weeks of age). Dosage: 10 mg/kg. Administration: Oral gavage; for 4 hours (Pharmacokinetic study). Result: Tissue concentrations decreased in the order liver > kidney > small intestine > spleen > brain.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Fisogatinib | BLU554

Quick Database Links

Gene Symbol

FGFR