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ChemicalBook--->CAS DataBase List--->1453208-66-6

1453208-66-6

1453208-66-6 Structure

1453208-66-6 Structure
IdentificationBack Directory
[Name]

ASP5878
[CAS]

1453208-66-6
[Synonyms]

ASP5878
ASP-5878 (ASP5878
ASP5878; ASP 5878; ASP-5878
[Molecular Formula]

C18H19F2N5O4
[MOL File]

1453208-66-6.mol
[Molecular Weight]

407.37
Chemical PropertiesBack Directory
[Boiling point ]

645.3±65.0 °C(Predicted)
[density ]

1.41±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : ≥ 250 mg/mL (613.69 mM);Water : < 0.1 mg/mL (insoluble)
[form ]

Solid
[pka]

14.41±0.10(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

ASP5878 is a selective inhibitor of FGFR1, 2, 3 and 4.
[in vivo]

ASP5878 (3 mg/kg, orally, once daily) shows antitumor activity in a Hep3B2.1-7 subcutaneous xenograft? and HCC orthotopic xenograft mouse model[1].
? ASP5878 induces shrinkage of FGF19-expressing HCC xenograft model[1].

Animal Model:Four-week-old male nude mice (CAnN.Cg-Foxn1nu/CrlCrlj [nu/nu]) (Hep3B2.1-7 cells inoculated subcutaneously)[1].
Dosage:3 mg/kg.
Administration:Orally once daily from days 14 to 52.
Result:Induced tumor regression by 9% and 88% at 1 and 3 mg/kg, respectively, without affecting the body weight for 14 days.
Induced the suppression of FGFR4 phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation.
Animal Model:HCC orthotopic xenograft model (mouse)[1].
Dosage:3 mg/kg.
Administration:Orally once daily for 24 days.
Result:Exhibited a lower tumor burden than vehicle- and sorafenibtreated mice.
Induced sustained tumor regression without tumor regrowth.
[IC 50]

FGFR1: 0.47 nM (IC50); FGFR2: 0.6 nM (IC50); FGFR3: 0.74 nM (IC50); FGFR4: 3.5 nM (IC50)
[storage]

Store at -20°C
Spectrum DetailBack Directory
[Spectrum Detail]

ASP5878(1453208-66-6)1HNMR
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