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ASP5878

Cat. No. M10518
ASP5878 Structure
Synonym:

ASP-5878

Size Price Availability Quantity
5mg USD 290  USD290 In stock
10mg USD 500  USD500 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

ASP5878 is a novel selective FGFR inhibitor with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3 and 4, respectively. 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, ASP5878 (3 mg/kg; oral administration) 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.

Protocol
Cell Experiment
Cell lines Human HCC cell lines
Preparation method HCC cell lines were cultured according to each manufacturer’s guideline. The cell lines in this study were not authenticated by any tests in our laboratory but were purchased from the providers of authenticated cell lines and stored at early passages in a central cell bank at Astellas Pharma Inc. 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-GloTM (Promega, Madison, WI).
Concentrations 0-1000 nM
Incubation time 5 days
Animal Experiment
Animal models HCC orthotopic xenograft model
Formulation Cremophor EL/ethanol or 0.5% MC
Dosages 3 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 407.37
Formula C18H19F2N5O4
CAS Number 1453208-66-6
Purity >99%
Solubility DMSO ≥ 80 mg/mL
Storage at -20°C
References

[1] Aya Kikuchi, et al. Cancer Sci. ASP5878, a selective FGFR inhibitor, to treat FGFR3-dependent urothelial cancer with or without chemoresistance

[2] Takashi Futami, et al. Mol Cancer Ther. ASP5878, a Novel Inhibitor of FGFR1, 2, 3, and 4, Inhibits the Growth of FGF19-Expressing Hepatocellular Carcinoma

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  Catalog
Abmole Inhibitor Catalog




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