Home Protein Tyrosine Kinase FGFR inhibitor ASP5878 For research use only.

ASP5878

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

ASP5878 Chemical Structure

CAS: 1453208-66-6

Selleck's ASP5878 has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.93%
99.93

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

--
In Vivo
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].
Animal Research Animal Models HCC orthotopic xenograft model
Dosages 3 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02038673 Completed Solid Tumors Astellas Pharma Inc|Astellas Pharma Global Development Inc. November 5 2013 Phase 1

Chemical lnformation & Solubility

Molecular Weight 407.37 Formula

C18H19F2N5O4
CAS No. 1453208-66-6 SDF --
Smiles COC1=CC(=C(C(=C1F)COC2=CN=C(N=C2)NC3=CN(N=C3)CCO)F)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 81 mg/mL ( (198.83 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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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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