Fisogatinib

SKU: orb1304186

Description

Fisogatinib

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1707289-21-1
• MW: 503.38
• Purity: 99.87% (May vary between batches)
• Formula: C₂₄H₂₄Cl₂N₄O₄
• SMILES: COc1cc(OC)c(Cl)c(c1Cl)-c1ccc2nc(N[C@@H]3COCC[C@@H]3NC(=O)C=C)ncc2c1
• Target: FGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:93 mg/mL (184.75 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.56 mM);Ethanol:2 mg/mL (3.97 mM)

Bioactivity

• Target IC50:
  FGFR4:5 nM
• In Vivo:
  METHODS: A preliminary experiment was conducted in which male wild-type and Oatp1a/1b−/− mice were given Fisogatinib (BLU-554) (10 mg/kg, oral) and the plasma concentration before 4 hours and the liver-to-plasma ratio at 4 hours were analyzed. RESULTS Oatp1a/1b protein had little effect on the oral efficacy or liver distribution of Fisogatinib (BLU-554) in mice.
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• In Vitro:
  METHODS: Transepithelial drug transport was assessed using polarized monolayers of MDCK-II parental cells and their subclones overexpressing hABCB1, hABCG2, or mAbcg2 treated with Fisogatinib (BLU-554) (5 μM). RESULTS Fisogatinib (BLU-554) was moderately transported by hABCB1 and slightly transported by mAbcg2.
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Storage & Handling

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

Alternative Names

inhibit, Inhibitor, Fisogatinib, Fibroblast growth factor receptor, FGFR, FGFR4, FGFR3, FGFR2, FGFR1, BLU 554, BLU554, BLU-554

Compound Identifiers

PubChem CID

91885617