Emvododstat (PTC299)

Catalog No.E1078 Batch:E107801

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Technical Data

Formula

C25H20Cl2N2O3
Molecular Weight 467.34 CAS No. 1256565-36-2
Solubility (25°C)* In vitro DMSO 93 mg/mL (198.99 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

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

Emvododstat has no adverse off‐target effects and no adverse effects on neurological or cardiopulmonary organ systems in rats and dogs[4].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    HeLa cells, leukemia cells

  • Concentrations

    0.1-1000 nM

  • Incubation Time

    72 h

  • Method

    Cells are treated with Emvododstat 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.
Animal Study:

[4]
  • Animal Models

    rats, dogs

  • Dosages

    0.03 to 3 mg/kg

  • Administration

    p.o.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.