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ASP5878 - 10mM in DMSO, high purity , CAS No.1453208-66-6, Inhibitor of fibroblast growth factor receptor 3
FGFR1 Selective Inhibitors
Basic Description
Synonyms
ASP5878 | ASP-5878 | 1453208-66-6 | Asp 5878 | ASP 5878 [WHO-DD] | C0Z095LL72 | 1H-Pyrazole-1-ethanol, 4-((5-((2,6-difluoro-3,5-dimethoxyphenyl)methoxy)-2-pyrimidinyl)amino)- | 1453208-66-6 (free base) | 2-(4-((5-((2,6-difluoro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amin
Specifications & Purity
Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms
ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively.
Storage Temp
Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of fibroblast growth factor receptor 3
Product Description
Information
ASP5878 is a novelFGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively.
Targets
FGFR1 (Cell-free assay); FGFR2 (Cell-free assay); FGFR3 (Cell-free assay); FGFR4 (Cell-free assay) 0.47 nM; 0.6 nM; 0.74 nM; 3.5 nM
In vitro
ASP5878 inhibits the cell proliferation of HCC cell lines expressing FGF19. ASP5878 inhibits FGFR4 phosphorylation and its treatment results in the suppression of phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation in Hep3B2.1-7 cells.
In vivo
Oral administration of ASP5878 at 3 mg/kg induces sustained tumor regression in a subcutaneous xenograft mouse model using Hep3B2.1-7. In HuH-7, an orthotopic xenograft mouse model, ASP5878 induces complete tumor regression and dramatically extended the survival of the mice.
Cell Research(from reference)
Cell lines：Hep3B2.1-7 cells
Concentrations：0-1000 nM
Incubation Time：2 h
Taxonomic Classification
Kingdom
Organic compounds
Superclass
Benzenoids
Class
Benzene and substituted derivatives
Subclass
Methoxybenzenes
Intermediate Tree Nodes
Not available
Direct Parent
Dimethoxybenzenes
Alternative Parents
Phenoxy compounds Anisoles Fluorobenzenes Aminopyrimidines and derivatives Alkyl aryl ethers Aryl fluorides Pyrazoles Heteroaromatic compounds Azacyclic compounds Alkanolamines Primary alcohols Organofluorides Hydrocarbon derivatives
Molecular Framework
Aromatic heteromonocyclic compounds
Substituents
M-dimethoxybenzene - Dimethoxybenzene - Phenoxy compound - Anisole - Phenol ether - Alkyl aryl ether - Aminopyrimidine - Fluorobenzene - Halobenzene - Aryl fluoride - Aryl halide - Pyrimidine - Pyrazole - Azole - Heteroaromatic compound - Organoheterocyclic compound - Alkanolamine - Ether - Azacycle - Organic nitrogen compound - Organohalogen compound - Organofluoride - Organonitrogen compound - Alcohol - Hydrocarbon derivative - Organic oxygen compound - Amine - Primary alcohol - Organooxygen compound - Aromatic heteromonocyclic compound
Description
This compound belongs to the class of organic compounds known as dimethoxybenzenes. These are organic aromatic compounds containing a monocyclic benzene moiety carrying exactly two methoxy groups.
External Descriptors
Not available
Data sources
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
Product Properties
ALogP
2.178
hba_count
6
HBD Count
2
Rotatable Bond
9
Associated Targets(Human)
Associated Targets(non-human)
Mechanisms of Action
Mechanism of Action
Action Type
target ID
Target Name
Target Type
Target Organism
Binding Site Name
References
Names and Identifiers
IUPAC Name
2-[4-[[5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl]amino]pyrazol-1-yl]ethanol
INCHI
InChI=1S/C18H19F2N5O4/c1-27-14-5-15(28-2)17(20)13(16(14)19)10-29-12-7-21-18(22-8-12)24-11-6-23-25(9-11)3-4-26/h5-9,26H,3-4,10H2,1-2H3,(H,21,22,24)
InChIKey
VDZZYOJYLLNBTD-UHFFFAOYSA-N
Smiles
COC1=CC(=C(C(=C1F)COC2=CN=C(N=C2)NC3=CN(N=C3)CCO)F)OC
Isomeric SMILES
COC1=CC(=C(C(=C1F)COC2=CN=C(N=C2)NC3=CN(N=C3)CCO)F)OC
Molecular Weight
407.37
Reaxy-Rn
26815998
Reaxys-RN_link_address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26815998&ln=
Certificates（CoA,COO,BSE/TSE and Analysis Chart)
Chemical and Physical Properties
DMSO(mg / mL) Max Solubility
81
DMSO(mM) Max Solubility
198.836438618455
Water(mg / mL) Max Solubility
＜1
Molecular Weight
407.400 g/mol
XLogP3
1.200
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
10
Rotatable Bond Count
9
Exact Mass
407.141 Da
Monoisotopic Mass
407.141 Da
Topological Polar Surface Area
104.000 Ų
Heavy Atom Count
29
Formal Charge
0
Complexity
473.000
Isotope Atom Count
0
Defined Atom Stereocenter Count
0
Undefined Atom Stereocenter Count
0
Defined Bond Stereocenter Count
0
Undefined Bond Stereocenter Count
0
The total count of all stereochemical bonds
0
Covalently-Bonded Unit Count
1
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