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Emvododstat (PTC299) VEGFR inhibitor

Name: Emvododstat (PTC299)
Brand: Selleck Chemicals
SKU: E1078
Availability: InStock
Rating: 5 (1 reviews)

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.

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%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS/MSDS
Datasheet

99.60

Related Targets	EGFR FGFR PDGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other VEGFR Inhibitors	SAR131675 SU 5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Anlotinib (AL3818) Dihydrochloride Linifanib (ABT-869) Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 Semaxanib (SU5416)

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (198.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.65mg/ml (9.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 93 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.66mg/ml (1.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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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.

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	1 year-80°Cin solvent 1 month-20°Cin solvent

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	Dihydroorotate dehydrogenase VEGFA (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.
In vivo	In rats and dogs, Emvododstat (PTC299) has no adverse off‐target effects and no adverse effects on neurological or cardiopulmonary organ systems.
References	[1] https://pubmed.ncbi.nlm.nih.gov/35151222/ [2] https://pubmed.ncbi.nlm.nih.gov/30352802/ [3] https://pubmed.ncbi.nlm.nih.gov/33249060/ [4] https://pubmed.ncbi.nlm.nih.gov/27310330/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2023-06-26)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04439071	TERMINATED	Pneumonia; COVID-19; Coronavirus	PTC Therapeutics	2020-07-09	PHASE2; PHASE3
NCT03761069	TERMINATED	Leukemia, Myeloid, Acute; AML	PTC Therapeutics	2018-10-29	PHASE1
NCT03761069	Terminated	Leukemia Myeloid Acute\|AML	PTC Therapeutics	2018-10-29	Phase 1
NCT01158300	COMPLETED	Brain and Central Nervous System Tumors	Pediatric Brain Tumor Consortium	2010-11	PHASE1
NCT00911248	TERMINATED	Neurofibromatosis 2	PTC Therapeutics	2009-07-31	PHASE2
NCT00508586	COMPLETED	Metastatic Breast Cancer	PTC Therapeutics	2007-11	PHASE1

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