ASP5878

SKU: orb1301762

Description

ASP5878 is a potent and selective pan-FGFR inhibitor, demonstrating low nanomolar IC50 values against FGFR1-4. This small molecule is a valuable research tool for investigating FGFR-driven signaling in both in vitro biochemical assays and in vivo cancer models, particularly for studying tumorigenesis and potential therapeutic interventions.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1453208-66-6
• MW: 407.37
• Purity: 99.89% (May vary between batches)
• Formula: C₁₈H₁₉F₂N₅O₄
• SMILES: COc1cc(OC)c(F)c(COc2cnc(Nc3cnn(CCO)c3)nc2)c1F
• Target: FGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (12.27 mM);DMSO:250 mg/mL (613.69 mM)

Bioactivity

• Target IC50:
  FGFR3:0.74nM|FGFR4:3.5nM|FGFR1:0.47nM|FGFR2:0.6nM
• In Vivo:
  sorafenib administration for 14 days caused 40% tumor growth inhibition in the Hep3B2.1-7 xenograft model. Even after continuous sorafenib treatment, the Hep3B2.1-7 tumor gradually enlarged, and 47% tumor growth inhibition was observed by day 31. In contrast, the switch from sorafenib to ASP5878 on day 14 induced 83% tumor regression on day 52 relative to the tumor size observed on day 14. This indicates the therapeutic potential of ASP5878 for FGF19-overexpressing HCC patients who previously received sorafenib treatment.
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• Cell Research:
  The human HCC cell lines, The experiments were conducted using low-passage cultures of these stocks. The cells were seeded in 96-well plates and incubated overnight. The cells were treated with ASP5878 for 5 days. Cell viability was measured using CellTiter-Glo.
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• Animal Research:
  HuH-7-Luc cells were inoculated into hepatic parenchyma at 3×10^5 cells/0.01 mL (Matrigel 100%)/mouse. One week after inoculation, the mice were divided into three groups (n = 5 per group) on day 0 on the basis of bioluminescent imaging. Vehicle (Cremophor EL/ethanol or 0.5% MC), sorafenib (30 mg/kg), or ASP5878 (3 mg/kg) was administered as a once-daily oral dose for 91 days. Tumor growth was monitored by in vivo bioluminescent imaging of the abdomen after intraperitoneally injecting luciferin using IVIS-Lumina2. During the study period (181 days), the survival of mice bearing hepatic tumors was recorded. The condition of the mice was monitored daily. The mice were scored as dead if any of the following signs of suffering were observed: cachexia, weakening, and difficulty in moving or eating. Mice that were scored as dead were euthanized.
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Storage & Handling

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

Alternative Names

inhibit, Fibroblast growth factor receptor, FGFR, FGFR4, FGFR1, FGFR3, FGFR2, Inhibitor, ASP 5878, ASP-5878, ASP5878

Compound Identifiers

PubChem CID

71736582