Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fisogatinib (BLU-554) is a potent inhibitor of fibroblast growth factor receptor 4 (FGFR4).
説明 | Fisogatinib (BLU-554) is a potent inhibitor of fibroblast growth factor receptor 4 (FGFR4). |
ターゲット&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]. |
キナーゼ試験 | 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]. |
別名 | BLU554, BLU 554, BLU-554 |
分子量 | 503.38 |
分子式 | C24H24Cl2N4O4 |
CAS No. | 1707289-21-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 2 mg/mL (3.97 mM)
DMSO: 93 mg/mL (184.8 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Fisogatinib 1707289-21-1 Angiogenesis Tyrosine Kinase/Adaptors FGFR inhibit BLU554 Fibroblast growth factor receptor BLU 554 BLU-554 Inhibitor inhibitor