Home Angiogenesis FGFR inhibitor Fisogatinib (BLU-554) For research use only.

Fisogatinib (BLU-554)

Fisogatinib (BLU-554) is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM.

Fisogatinib (BLU-554) Chemical Structure

Fisogatinib (BLU-554) Chemical Structure

CAS No. 1707289-21-1

Purity & Quality Control

Fisogatinib (BLU-554) Related Products

Signaling Pathway

FGFR Signaling Pathways

FGFR Signaling Pathway

Biological Activity

Description Fisogatinib (BLU-554) is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM.
Targets
FGFR4 [1]
(Cell-free assay)
5 nM
In vitro
In vitro

BLU-554 exploits a unique interaction with FGFR4 to confer potency and selectivity
Cell Research Cell lines ST8814 resistant cells
Concentrations 1 µM
Incubation Time 4 h
Method

ST8814 resistant cells were treated with DMSO or BLU-554 at 1 µM for 4 hrs.
In Vivo
In vivo

BLU-554 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models[1].
Animal Research Animal Models Male FVB/NRj mice
Dosages 10 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02508467 Completed
Hepatocellular Carcinoma (HCC)
Blueprint Medicines Corporation
 July 31 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 503.38 Formula

C24H24Cl2N4O4
CAS No. 1707289-21-1 SDF Download Fisogatinib (BLU-554) SDF
Smiles COC1=CC(=C(C(=C1Cl)C2=CC3=CN=C(N=C3C=C2)NC4COCCC4NC(=O)C=C)Cl)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (198.65 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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