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Fisogatinib

Catalog No. T3456   CAS 1707289-21-1
Synonyms: BLU554, BLU 554, BLU-554

Fisogatinib (BLU-554) is a potent inhibitor of fibroblast growth factor receptor 4 (FGFR4).

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Fisogatinib Chemical Structure
Fisogatinib, CAS 1707289-21-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 51.00
2 mg In stock $ 73.00
5 mg In stock $ 122.00
10 mg In stock $ 197.00
25 mg In stock $ 378.00
50 mg In stock $ 569.00
100 mg In stock $ 819.00
500 mg In stock $ 1,690.00
1 mL * 10 mM (in DMSO) In stock $ 135.00
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Purity: 99.42%
Purity: 99.27%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Fisogatinib (BLU-554) is a potent inhibitor of fibroblast growth factor receptor 4 (FGFR4).
Targets&IC50 FGFR4:5 nM
In vitro BLU-554 exploits a unique interaction with FGFR4 to confer potency and selectivity
In vivo BLU-554 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models[1].
Kinase Assay The Ki value and mode of inhibition of LY2801653 for the MET kinase activity are determined using a radiometric filter-binding assay. Reactions are carried out in 96-well plates in Enzyme dilution buffer (EDB) compose of 50 mM Tris HCl pH 7.5, 2 mM DTT, 0.005% Triton X-100, 10 mM MgCl2, and 250 ?M EDTA. Serially diluted LY2801653 (final concentration 250 to 0 nM) are followed by the addition of a series of 8 concentrations of 33P-γ-ATP (final concentration 400 to 10 μM ATP), and 5 nM enzyme (final concentration). After a 2-hour incubation, PolyGluTyr synthetic protein substrate (final 150 μg/mL) is added to initiate the 30-minute kinase reaction. Reactions are quenched with 10% H3PO4, transfer to a pre-wetted Multiscreen anionic phosphocellulose 96-well filter plate, and washed; radioactivity is measured with a scintillation counter. The experimental data are fit to a global mix model inhibition equation using GraphPad Prism softwar to generate an alpha value to determine the modality of inhibition and to calculate the Ki value for LY2801653[1].
Synonyms BLU554, BLU 554, BLU-554
Molecular Weight 503.38
Formula C24H24Cl2N4O4
CAS No. 1707289-21-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 2 mg/mL (3.97 mM)

DMSO: 93 mg/mL (184.8 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Blueprint Medicines. 50th th international liver congress. 2015.

TargetMolCitations

1. Tao Z, Cui Y, Xu X, et al. FGFR redundancy limits the efficacy of FGFR4-selective inhibitors in hepatocellular carcinoma. Proceedings of the National Academy of Sciences. 2022, 119(40): e2208844119.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Highly Selective Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library ReFRAME Related Library Anti-Breast Cancer Compound Library

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Related compounds with same targets
Sucralfate FGFR3-IN-7 ENMD-2076 ZM323881 hydrochloride Nintedanib esylate Pazopanib Hydrochloride Futibatinib CP-547632 hydrochloride

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Keywords

Fisogatinib 1707289-21-1 Angiogenesis Tyrosine Kinase/Adaptors FGFR inhibit BLU554 Fibroblast growth factor receptor BLU 554 BLU-554 Inhibitor inhibitor

 

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