Cat. No.: HY-100492

Fisogatinib

(Synonyms: BLU-554)

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

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.

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Pureté: 99.70%
CAS No.: 1707289-21-1
Formule: C₂₄H₂₄Cl₂N₄O₄
Masse moléculaire:503.38

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Fisogatinib Chemical Structure

CAS No.: 1707289-21-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Essai clinique
Chemical Information
Publications (5)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

FGFR4

5 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	66.5 nM Compound: BLU-554	Antiproliferative activity against mouse BaF3 cells expressing TEL-FGFR4 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells expressing TEL-FGFR4 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35635004]
BaF3	IC₅₀	0.396 μM Compound: BLU-554	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-FGFR4-V550L mutant measured after 24 to 48 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring ETV6-FGFR4-V550L mutant measured after 24 to 48 hrs by MTT assay	[PMID: 37437349]
BaF3	IC₅₀	0.528 μM Compound: BLU-554	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-FGFR4-N535K mutant measured after 24 to 48 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring ETV6-FGFR4-N535K mutant measured after 24 to 48 hrs by MTT assay	[PMID: 37437349]
BaF3	IC₅₀	>2000 nM Compound: 1; BLU554	Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]
BaF3	IC₅₀	>2000 nM Compound: 1; BLU554	Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]
BaF3	IC₅₀	9.2 nM Compound: 1; BLU554	Antiproliferative activity against mouse BaF3 cells harboring wild type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring wild type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]
Hep 3B2	IC₅₀	40 nM Compound: BLU-554	Antiproliferative activity against human Hep3B cells expressing FGF19/FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Hep3B cells expressing FGF19/FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35635004]
Hep 3B2	IC₅₀	0.046 μM Compound: BLU-554	Antiproliferative activity against human Hep3B cells measured after 24 to 48 hrs by MTT assay Antiproliferative activity against human Hep3B cells measured after 24 to 48 hrs by MTT assay	[PMID: 37437349]
Hep 3B2	IC₅₀	122 nM Compound: 8	Antiproliferative activity against FGF19 amplified human Hep3B cells assessed as inhibition of cell growth by SRB assay Antiproliferative activity against FGF19 amplified human Hep3B cells assessed as inhibition of cell growth by SRB assay	[PMID: 38706130]
HepG2	IC₅₀	4.431 μM Compound: BLU-554	Antiproliferative activity against human HepG2 cells measured after 24 to 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells measured after 24 to 48 hrs by MTT assay	[PMID: 37437349]
Huh-7	IC₅₀	50 nM Compound: BLU-554	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35635004]
Huh-7	IC₅₀	45.9 nM Compound: 4	Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay	[PMID: 36480917]
Huh-7	IC₅₀	81 nM Compound: BLU-554	Antiproliferative activity against human Huh-7 cells measured after 24 to 48 hrs by MTT assay Antiproliferative activity against human Huh-7 cells measured after 24 to 48 hrs by MTT assay	[PMID: 37437349]
Huh-7	IC₅₀	81 nM Compound: 8	Antiproliferative activity against FGFR4 overexpressing human Huh-7 cells assessed as inhibition of cell growth by SRB assay Antiproliferative activity against FGFR4 overexpressing human Huh-7 cells assessed as inhibition of cell growth by SRB assay	[PMID: 38706130]
L02	IC₅₀	>10 μM Compound: BLU-554	Antiproliferative activity against human L02 cells measured after 24 to 48 hrs by MTT assay Antiproliferative activity against human L02 cells measured after 24 to 48 hrs by MTT assay	[PMID: 37437349]
NCI-H1581	IC₅₀	>1000 nM Compound: BLU-554	Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35635004]
RT-112	IC₅₀	>1000 nM Compound: BLU-554	Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35635004]
SNU-16	IC₅₀	>1000 nM Compound: BLU-554	Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35635004]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1707289-21-1
Appearance Solid
Masse moléculaire 503.38
Formule C₂₄H₂₄Cl₂N₄O₄
Color White to light yellow
SMILES

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

BLU-554
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

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Nat Genet

Multiparametric and accurate functional analysis of genetic sequence variants using CRISPR-Select. [Abstract]

2022 Dec;54(12):1983-1993. PMID: 36471068
Fundam Res

2026 Mar 12.
Int Immunopharmacol

FGFR4 inhibition augments paclitaxel-induced cell death in ovarian cancer. [Abstract]

2025 Apr 16:155:114626. PMID: 40245772
J Endocrinol Invest

Bromocriptine sensitivity in bromocriptine-induced drug-resistant prolactinomas is restored by inhibiting FGF19/FGFR4/PRL. [Abstract]

2025 Jan;48(1):67-80. PMID: 38926262
University of Auckland

2025.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (198.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Dogan-Topal B, et al. Quantification of FGFR4 inhibitor BLU-554 in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Mar 15;1110-1111:116-123. [Content Brief]

[2]. Richard Kim, et al. First-in-human study of BLU-554, a potent, highly selective FGFR4 inhibitor designed for hepatocellular carcinoma (HCC) with FGFR4 pathway activation. EJC. December 2016, Volume 69, Supplement 1, Page S41.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9866 mL	9.9329 mL	19.8657 mL	49.6643 mL
	5 mM	0.3973 mL	1.9866 mL	3.9731 mL	9.9329 mL
	10 mM	0.1987 mL	0.9933 mL	1.9866 mL	4.9664 mL
	15 mM	0.1324 mL	0.6622 mL	1.3244 mL	3.3110 mL
	20 mM	0.0993 mL	0.4966 mL	0.9933 mL	2.4832 mL
	25 mM	0.0795 mL	0.3973 mL	0.7946 mL	1.9866 mL
	30 mM	0.0662 mL	0.3311 mL	0.6622 mL	1.6555 mL
	40 mM	0.0497 mL	0.2483 mL	0.4966 mL	1.2416 mL
	50 mM	0.0397 mL	0.1987 mL	0.3973 mL	0.9933 mL
	60 mM	0.0331 mL	0.1655 mL	0.3311 mL	0.8277 mL
	80 mM	0.0248 mL	0.1242 mL	0.2483 mL	0.6208 mL
	100 mM	0.0199 mL	0.0993 mL	0.1987 mL	0.4966 mL

Keywords

Fisogatinib

5 Cited Publications

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Fisogatinib

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Protein Tyrosine Kinase Compound Library

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Anti-Lung Cancer Compound Library

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Publications Citing Use of MedChemExpress (MCE) Fisogatinib

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Fisogatinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Fisogatinib

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Fisogatinib Related Classifications

HY-100492 Related Classifications