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

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Emvododstat (PTC299) VEGFR inhibitor

Cat.No.E1078

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

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 467.34 Formula

C25H20Cl2N2O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1256565-36-2 -- Storage of Stock Solutions

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Mechanism of Action

Targets/IC50/Ki
Dihydroorotate dehydrogenase [1]
VEGFA [2]
(in hypoxia-induced VEGFA protein inhibition assay of HeLa cells)
1.64 nM(EC50)
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]
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].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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