Roxadustat (FG-4592)

Catalog No.S1007 Synonyms: ASP1517

Roxadustat (FG-4592) Chemical Structure

Molecular Weight(MW): 352.34

Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Phase 3.

Size Price Stock Quantity  
In DMSO USD 64 In stock
USD 70 In stock
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Cited by 14 Publications

6 Customer Reviews

  • Immunoblots showing dose-dependent HIF-1α stabilization in U2OS, HeLa and Hep3b (and HIF-2α) cells after 6 hours treatment with FG-4592.

    Chem Sci, 2017, doi: 10.1039/C7SC02103H. Roxadustat (FG-4592) purchased from Selleck.

  • (A) The viability of the EpSCs in each group was detected by CCK-8 assays. The EpSCs were under the indicated conditions for 24 h. The viability of each group is shown as the mean±SD. *, P<0.05 versus the normoxia control group; #, P<0.05 versus the hypoxia control group. (B) Western blotting results showing that FG-4592 simulated hypoxia-induced increases in HIF-1α and PCNA expression.

    Cell Physiol Biochem, 2018, 46(6):2460-2470. Roxadustat (FG-4592) purchased from Selleck.

  • Blood urea nitrogen (A), serum creatinine (B) and serum cystatin C (C) levels. Data were presented as means ± SD (n = 8 in each group). (D) Representative images of periodic acid-Schiff staining (upper: ×100, lower: ×400) of kidneys. (E) Tubular injury score in mice. Data were presented asmeans ± SD of 10 random fields from each kidney (n = 8 in each group).

    Clin Sci, 2018, 132(7):825-838. Roxadustat (FG-4592) purchased from Selleck.

  • (B and C) Luciferase reporter activity following treatment with CP-312 or known HIF inducers, FG-4592 and BAY 85-3934, in (B) HIF-1 MIA PaCa-2 and (C) HIF-2-specific PANC-1 luciferase reporter cell lines.

    J Pharmacol Exp Ther, 2018, 364(1):87-96. Roxadustat (FG-4592) purchased from Selleck.

  • Protein content of Hypoxia-inducible factor 1, alpha subunit (HIF-1α) of PC12 cells treated with tert-Butyl hydroperoxide (TBHP) and TBHP plus FG-4592.

    Brain Res, 2016, 1632:19-26. Roxadustat (FG-4592) purchased from Selleck.

  • Roxadustat (FG-4592) increases the differentiation of ADMSCs in hypoxic conditions. Representative micrographs showing immunofluorescence of COL I(green) and HIF-1a(green), and DAPI-labelled nuclei(blue) in each group. All cells were detected at day 21 post-induction.

    Cell Prolif, 2016, 49(2):173-84.. Roxadustat (FG-4592) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Phase 3.
Targets
HIF α prolyl hydroxylase [1]
(Cell-free assay)
In vitro

FG-4592 is an oral inhibitor of hypoxia inducible factor (HIF) prolyl hydroxylase currently in clinical development for the treatment of anemia. FG-4592 stabilizes the activities of HIF, a cytosolic transcription factor, leading to activation of the genes associated with erythropoiesis, including erythropoietin and enzymes involved in iron metabolism. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EpSC cell NH6wUFRE\WyuII\pZYJqdGm2eTDhd5NigQ>? NY\ZOJBlPSEEtV2gc5IhOTBiwsXN NX3vWJY6OjRiaB?= NE[4RWRHTy12NUmyJIlv[3KnYYPl[EBGeFOFIHPlcIwhfmmjYnnsbZR6KGmwIH7vdo1wgGmjLh?= NUG4SJpxOjl5NEK0PVg>
Adiposederived mesenchymal stem cells (ADMSCs) NYXlenU6TnWwY4Tpc44h[XO|YYm= MljMOUDPxE1? MVf0bIUhdGW4ZXygc4YhUEmILUHhJIV5eHKnc4Ppc44hf2G|IH31Z4ghcGmpaHXyJIlvKHSqZTDGS{01PTl{LYTy[YF1\WRiZ4LveZAhfGijbjDpckB1cGVidnXobYNt\XS{ZXH0[YQh\3KxdYCu NU\mN5RkOjdyMkGyN|M>

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 70 mg/mL (198.67 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+50% PEG 300+ddH2O
For best results, use promptly after mixing.
11mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 352.34
Formula

C19H16N2O5

CAS No. 808118-40-3
Storage powder
in solvent
Synonyms ASP1517

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03303066 Recruiting Primary MDS Classified as Very Low Low or Intermediate Risk With <5% Blasts FibroGen|AstraZeneca June 6 2018 Phase 2|Phase 3
NCT03303066 Recruiting Primary MDS Classified as Very Low Low or Intermediate Risk With <5% Blasts FibroGen|AstraZeneca June 6 2018 Phase 2|Phase 3
NCT03263091 Recruiting Primary MDS (Very Low Low or Intermediate IPSS-R With <5% Blasts) FibroGen|AstraZeneca September 7 2017 Phase 3
NCT03263091 Recruiting Primary MDS (Very Low Low or Intermediate IPSS-R With <5% Blasts) FibroGen|AstraZeneca September 7 2017 Phase 3
NCT02952040 Completed Healthy Subjects Astellas Pharma Inc|FibroGen November 2016 Phase 1
NCT02952040 Completed Healthy Subjects Astellas Pharma Inc|FibroGen November 2016 Phase 1

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

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Can you tell me what the half-life of the product is, please?

  • Answer:

    The half-life of S1007 Roxadustat is around 12 hours. Please the reference below: https://www.ncbi.nlm.nih.gov/pubmed/26846333

HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID