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Fisogatinib (BLU-554) - 98%, high purity , CAS No.1707289-21-1, Inhibitor of fibroblast growth factor receptor 4
Basic Description Synonyms BLU-554|Fisogatinib|1707289-21-1|N-((3S,4S)-3-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)tetrahydro-2H-pyran-4-yl)acrylamide|BLU554|BLU111362|Fisogatinib [INN]|Fisogatinib [USAN]|BLU554(Fisogatinib)|X439161|BLU-111362|5Q7R99CKV2|BLU 554|X Specifications & Purity Moligand™, ≥98% Biochemical and Physiological Mechanisms 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. Storage Temp Store at -20°C Shipped In Ice chest + Ice pads Grade Moligand™ Action Type INHIBITOR Mechanism of action Inhibitor of fibroblast growth factor receptor 4 Product Description Information
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.
Targets
FGFR4 (Cell-free assay) 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.
Product Properties ALogP 4.229 HBD Count 2 Rotatable Bond 7
Names and Identifiers IUPAC Name N-[(3S,4S)-3-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]oxan-4-yl]prop-2-enamide INCHI InChI=1S/C24H24Cl2N4O4/c1-4-20(31)28-16-7-8-34-12-17(16)30-24-27-11-14-9-13(5-6-15(14)29-24)21-22(25)18(32-2)10-19(33-3)23(21)26/h4-6,9-11,16-17H,1,7-8,12H2,2-3H3,(H,28,31)(H,27,29,30)/t16-,17+/m0/s1 InChi Key MGZKYOAQVGSSGC-DLBZAZTESA-N Canonical SMILES COC1=CC(=C(C(=C1Cl)C2=CC3=CN=C(N=C3C=C2)NC4COCCC4NC(=O)C=C)Cl)OC Isomeric SMILES COC1=CC(=C(C(=C1Cl)C2=CC3=CN=C(N=C3C=C2)N[C@@H]4COCC[C@@H]4NC(=O)C=C)Cl)OC PubChem CID 91885617 Molecular Weight 503.38
Chemical and Physical Properties Solubility Solubility (25°C) In vitro DMSO: 100 mg/mL warmed with 50ºC Water: bath (198.65 mM); Ethanol: 2 mg/mL warmed with 50ºC Water: bath (3.97 mM); Water: Insoluble; DMSO(mg / mL) Max Solubility 100 DMSO(mM) Max Solubility 198.6570782 Water(mg / mL) Max Solubility ＜1
Safety and Hazards(GHS) Pictogram(s) GHS07 Signal Warning Hazard Statements H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
Precautionary Statements P261: Avoid breathing dust/fume/gas/mist/vapors/spray.
P305+P351+P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.
References 1. Yee NS. (2018) Update in Systemic and Targeted Therapies in Gastrointestinal Oncology.. Biomedicines, 6 (1): (589-97). [PMID:29547556 ]
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