All AbMole products are for research use only, cannot be used for human consumption.
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.
| 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 |
| Molecular Weight | 407.37 |
| Formula | C18H19F2N5O4 |
| CAS Number | 1453208-66-6 |
| Solubility (25°C) | DMSO ≥ 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related FGFR Products |
|---|
| SNIPER(TACC3)-11
SNIPER(TACC3)-11 is a potent FGFR3-TACC3 degrader. |
| LY-3076226
LY-3076226 is an antibody drug coupling (ADC) with a cleavable linker targeting FGFR2. |
| Aprutumab ixadotin
Aprutumab ixadotin is an antibody drug coupling (ADC) with a non-cleavable linker that targets FGFR2. |
| Gunagratinib
Gunagratinib is an orally active, potent, selective, and irreversible fibroblast growth factor receptor (pan-FGFR) inhibitor for use in cancer research. |
| SAR-442501
SAR-442501 is a novel anti-FGFR3 monoclonal antibody for studies related to achondroplasia (ACH). |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
