Chemical Properties | Back 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 Information | Back 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.
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| [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 |
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Company Name: |
BOC Sciences
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Tel: |
1-631-485-4226; 16314854226 |
Website: |
https://www.bocsci.com |
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