Fisogatinib (Synonyms: BLU-554)

Name: Fisogatinib
Brand: MedChemExpress
SKU: HY-100492
Rating: 5.0 (2 reviews)

Cat. No.: HY-100492 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1707289-21-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 166	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 166	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Fisogatinib

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Biological Activity
Purity & Documentation
References
Customer Review

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]
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]
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	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]
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.

Clinical Trial

Molecular Weight

503.38

Formula

C₂₄H₂₄Cl₂N₄O₄

CAS No.

1707289-21-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (250 KB) LCMS (110 KB)

Handling Instructions (2659 KB)

References

[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.

Complete Stock Solution Preparation Table

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

Fisogatinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fisogatinib1707289-21-1BLU-554BLU554BLU 554FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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Fisogatinib (Synonyms: BLU-554)

Customer Review

Fisogatinib Related Antibodies

2 Publications Citing Use of MCE Fisogatinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All FGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Fisogatinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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