Roxadustat (FG-4592)

Catalog No.S1007 Synonyms: ASP1517

For research use only.

Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Roxadustat potentiates RSL3 induced ferroptosis. Phase 3.

Roxadustat (FG-4592) Chemical Structure

CAS No. 808118-40-3

Selleck's Roxadustat (FG-4592) has been cited by 70 publications

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. Roxadustat potentiates RSL3 induced ferroptosis. 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 M2Lv[WNmdGxidnnhZoltcXS7IHHzd4F6 NIXhWnA2KML3TTDvdkAyOCEEtV2= MWOyOEBp NEXU[|lHTy12NUmyJIlv[3KnYYPl[EBGeFOFIHPlcIwhfmmjYnnsbZR6KGmwIH7vdo1wgGmjLh?= MkTIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NEK0PVgoRjJ7N{SyOFk5RC:jPh?=
Adiposederived mesenchymal stem cells (ADMSCs) MV;GeY5kfGmxbjDhd5NigQ>? MYO1JO69VQ>? NHXYO4N1cGVibHX2[Ywhd2ZiSFnGMVFiKGW6cILld5Nqd25id3HzJI12[2hiaHnnbIVzKGmwIITo[UBHTy12NUmyMZRz\WG2ZXSg[5JwfXBidHjhckBqdiC2aHWgeoVpcWOuZYTy[YF1\WRiZ4LveZAv M4nlWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEKxNlM{Lz5{N{CyNVI{OzxxYU6=
Hep3B NE\mXHBHfW6ldHnvckBie3OjeR?= M2P2TVUxKHSxIEK1NEB2VQ>? NXLZVmtKOTBiaILz NGP5RVJKdmirYnn0bY9vKG:oIFjJSk1RUER{IHnuJIh2dWGwIFjldFNDKGOnbHzzJIF{e2W|c3XkJIF{KEiLRj2xZYxxcGFicILveIVqdiC|dHHibYxqgmG2aX;uJIF1KDVyIITvJFI2OCC3TTDh[pRmeiBzMDDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?= Mnn6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NU[2NlMoRjJ7OEW2OlI{RC:jPh?=
Hep3B NGHXb4JHfW6ldHnvckBie3OjeR?= M2fie|UxKHSxIEK1NEB2VQ>? NIezcHkyOCCqcoO= NWr0THY2UW6qaXLpeIlwdiCxZjDITWYuWEiGMjDpckBpfW2jbjDI[ZA{SiClZXzsd{Bie3Onc4Pl[EBieyCKSV[tNoFteGijIIDyc5RmcW5ic4ThZoltcXqjdHnvckBifCB3MDD0c{AzPTBidV2gZYZ1\XJiMUCgbJJ{KGK7IGfld5Rmem5iYnzveEBu\XSqb3S= M3jWSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEW2OlI{Lz5{OUi1OlYzOzxxYU6=
Hep3B NVLpUFc5TnWwY4Tpc44h[XO|YYm= MX[1NEB2VQ>? NUjZXpF3OTBiaILz NXjr[4loUW6qaXLpeIlwdiCxZjDITWYuWEiGMjDpckBpfW2jbjDI[ZA{SiClZXzsd{Bie3Onc4Pl[EBieyC3cILl[5Vt[XSrb36gc4YhTVCRIH3SUmEhdGW4ZXygZZQhPTBidV2gZYZ1\XJiMUCgbJJ{KGK7IGLUMXBEWiCvZYToc4Q> MnXMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NU[2NlMoRjJ7OEW2OlI{RC:jPh?=
Assay
Methods Test Index PMID
Western blot HIF-α ; CA9 / NDRG1 / GLUT1 / GLUT3 / HK2 / PHD2 / JMJD1A / JMJD2B / JMJD2C 30334352 30801039

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.

10mg/mL

Chemical Information

Molecular Weight 352.34
Formula

C19H16N2O5

CAS No. 808118-40-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C2C=C(C=CC2=C(C(=N1)C(=O)NCC(=O)O)O)OC3=CC=CC=C3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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|Astellas Pharma Inc September 7 2017 Phase 3
NCT02988973 Completed 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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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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

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