ASP-5878

SKU: orb1220940

Description

ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1 2 3 and 4 with IC50 values of 0.47 0.60 0.74 and 3.5 nmol/L.

Key Properties

• CAS Number: 1453208-66-6
• MW: 407.38
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₉F₂N₅O₄
• SMILES: COc1cc(OC)c(F)c(COc2cnc(Nc3cnn(CCO)c3)nc2)c1F
• Target: FGFR
• Solubility: DMSO:250 mg/mL (613.69 mM)

Bioactivity

• In Vivo:
  Animal model: Four-week-old male nude mice (CAnN. Cg-Foxn1nu/CrlCrlj [nu/nu]) (Hep3B2.1-7 cells inoculated subcutaneously). 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). 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.
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• In Vitro:
  Cell Viability Assay Cell line: Human HCC cell lines. Concentration: 0-1000 nM. Incubation time: 5 days. Result: HuH-7, Hep3B2.1-7, and JHH-7 cell lines exhibited potent sensitivity to ASP5878, with IC50 values of 27, 8.5, and 21 nmol/L, respectively. The growth inhibition rate of HLF was 64% and those of other ASP5878-sensitive cell lines were higher than 95% at 1000 nM.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

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Gene Symbol

FGFR