ASP5878

Catalog No.S6539

For research use only.

ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively.

ASP5878 Chemical Structure

CAS No. 1453208-66-6

Selleck's ASP5878 has been cited by 3 Publications

Purity & Quality Control

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Biological Activity

Description ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively.
Targets
FGFR1 [1]
(Cell-free assay)
FGFR2 [1]
(Cell-free assay)
FGFR3 [1]
(Cell-free assay)
FGFR4 [1]
(Cell-free assay)
0.47 nM 0.6 nM 0.74 nM 3.5 nM
In vitro

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[1].

In vivo

Oral administration of ASP5878 at 3 mg/kg 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[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: Hep3B2.1-7 cells
  • Concentrations: 0-1000 nM
  • Incubation Time: 2 h
  • Method:

    --

Animal Research:

[1]

  • Animal Models: HCC orthotopic xenograft model
  • Dosages: 3 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 407.37
Formula

C18H19F2N5O4

CAS No. 1453208-66-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC(=C(C(=C1F)COC2=CN=C(N=C2)NC3=CN(N=C3)CCO)F)OC

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02038673 Completed Drug: ASP5878 Solid Tumors Astellas Pharma Inc|Astellas Pharma Global Development Inc. November 5 2013 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-11-29)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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