Home Protein Tyrosine Kinase VEGFR inhibitor - Dehydrogenase inhibitor Emvododstat (PTC299)

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Emvododstat (PTC299) VEGFR inhibitor

Emvododstat (PTC299) is a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), which inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells, this compound inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM.

Emvododstat (PTC299) VEGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 467.34

Purity & Quality Control

Batch: E107801 DMSO]93 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.60%
99.60

Related Products

Signaling Pathway

VEGFR Signaling Pathways

VEGFR Signaling Pathway

Mechanism of Action

Targets
Dihydroorotate dehydrogenase [1] VEGFA [2]
(in hypoxia-induced VEGFA protein inhibition assay of HeLa cells)
1.64 nM(EC50)

In vitro
In vitro

Emvododstat (PTC299) inhibits hypoxia-induced VEGFA protein production in HeLa cells with an EC50 of 1.64 ± 0.83 nM. It is the most potent inhibitor with an IC50 of about 1 nM, over 10 to 1000-fold more potent than Brequinar, Vidofludimus or A77-1726 in leukemia cells. The decreased translation of VEGFA mRNA by this compound is linked to the inhibition of de novo pyrimidine nucleotide synthesis as exogenously added uridine, but not other nucleosides, can completely block the inhibition of VEGFA production by Emvododstat.[2]
Cell Research Cell lines HeLa cells, leukemia cells
Concentrations 0.1-1000 nM
Incubation Time 72 h
Method

Emvododstat (PTC299) is used to treat cells at a series of doses for 72 hours, and the inhibition of cell proliferation is determined using a standard assay, CellTiter-Glo Luminescent Cell Viability Assay measures total cellular adenosine triphosphate (ATP) concentrations as an indicator of cell viability.

In Vivo
In vivo

In rats and dogs, Emvododstat (PTC299) has no adverse off‐target effects and no adverse effects on neurological or cardiopulmonary organ systems[4].
Animal Research Animal Models rats, dogs
Dosages 0.03 to 3 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03761069 Terminated
Leukemia Myeloid Acute|AML
PTC Therapeutics
 October 29 2018 Phase 1
NCT00911248 Terminated
Neurofibromatosis 2
PTC Therapeutics|United States Department of Defense
 July 31 2009 Phase 2
NCT00704821 Terminated
Advanced Cancer
PTC Therapeutics
 July 3 2008 Phase 1

References
  • https://pubmed.ncbi.nlm.nih.gov/35151222/
  • https://pubmed.ncbi.nlm.nih.gov/30352802/
  • https://pubmed.ncbi.nlm.nih.gov/33249060/
  • https://pubmed.ncbi.nlm.nih.gov/27310330/

Chemical Information

Molecular Weight 467.34 Formula

C25H20Cl2N2O3
CAS No. 1256565-36-2 SDF --
Smiles COC1=CC=C(C=C1)C2N(CCC3=C2[NH]C4=C3C=C(Cl)C=C4)C(=O)OC5=CC=C(Cl)C=C5

Storage and Stability

Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 93 mg/mL ( (198.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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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.
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
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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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