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 22 Publications

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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 NXzDUZpyS2WubDD2bYFjcWyrdImgZZN{[Xl? MkT6OUDDvU1ib4KgNVAhyrWP MoTCNlQhcA>? NHfk[2RHTy12NUmyJIlv[3KnYYPl[EBGeFOFIHPlcIwhfmmjYnnsbZR6KGmwIH7vdo1wgGmjLh?= NVrUPFd{Ojl5NEK0PVg>
Adiposederived mesenchymal stem cells (ADMSCs) NWDxbm8xTnWwY4Tpc44h[XO|YYm= MVS1JO69VQ>? M{jKbZRp\SCuZY\lcEBw\iCKSV[tNYEh\XiycnXzd4lwdiC5YYOgcZVkcCCqaXfo[ZIhcW5idHjlJGZINTR3OUKteJJm[XSnZDDndo92eCC2aHHuJIlvKHSqZTD2[Yhq[2yndILlZZRm\CCpcn;1dE4> MVqyO|AzOTJ|Mx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
HIF-α; 

PubMed: 30334352     


The effects of FG‐4592 on HIF1‐α were detected using Western Blot. Level of HIF‐1α was measured at different time points after the treatment of FG-4592.

CA9 / NDRG1 / GLUT1 / GLUT3 / HK2 / PHD2 / JMJD1A / JMJD2B / JMJD2C ; 

PubMed: 30801039     


0.05% DMSO (vehicle control), 1% O 2 (hypoxia), 100 µM VH298 and 50 µM FG-4592 were introduced to HeLa or HFF for 24 hours. Protein levels were analysed by immunoblotting using antibodies against indicated proteins, with β-Actin as loading control. The blots shown are representative of three independent experiments. * indicates longer exposure.

30334352 30801039

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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03303066 Recruiting Drug: FG-4592|Drug: Placebo Primary MDS Classified as Very Low Low or Intermediate Risk With <5% Blasts FibroGen|AstraZeneca June 6 2018 Phase 2|Phase 3
NCT03263091 Recruiting Drug: FG-4592|Drug: Placebo Primary MDS (Very Low Low or Intermediate IPSS-R With <5% Blasts) FibroGen|AstraZeneca September 7 2017 Phase 3
NCT02988973 Active not recruiting Drug: roxadustat|Drug: DA Chronic Kidney Disease Astellas Pharma Inc|FibroGen January 12 2017 Phase 3
NCT02964936 Completed Drug: roxadustat Chronic Kidney Disease Astellas Pharma Inc|FibroGen January 11 2017 Phase 3
NCT02952040 Completed Drug: ASP1517|Drug: Lanthanum carbonate hydrate Healthy Subjects Astellas Pharma Inc|FibroGen November 2016 Phase 1
NCT02952092 Completed Drug: roxadustat|Drug: Darbepoetin alfa Hemodialysis Chronic Kidney Disease Patients With Anemia Astellas Pharma Inc|FibroGen November 30 2016 Phase 3

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