1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. Fisogatinib

Fisogatinib (Synonyms: BLU-554)

Cat. No.: HY-100492 Purity: 99.84%
Handling Instructions

Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling.

For research use only. We do not sell to patients.

Fisogatinib Chemical Structure

Fisogatinib Chemical Structure

CAS No. : 1707289-21-1

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10 mM * 1 mL in DMSO USD 166 In-stock
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50 mg USD 750 In-stock
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100 mg USD 1300 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling[1][2].

IC50 & Target[1]

FGFR4

5 nM (IC50)

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[1].

Animal Model: Wild type male mice(FVB/NRj, 11-14 weeks of age)[1]
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.
Clinical Trial
Molecular Weight

503.38

Formula

C₂₄H₂₄Cl₂N₄O₄

CAS No.

1707289-21-1

SMILES

C=CC(N[[email protected]@H]1[[email protected]](NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)COCC1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (49.66 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9866 mL 9.9329 mL 19.8657 mL
5 mM 0.3973 mL 1.9866 mL 3.9731 mL
10 mM 0.1987 mL 0.9933 mL 1.9866 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.84%

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Keywords:

FisogatinibBLU-554BLU554BLU 554FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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Product name:
Fisogatinib
Cat. No.:
HY-100492
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