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PTC299

CAT: 0804-HY-124593-03Size: 10 mM - 1 mLDry Ice: NoHazardous: No
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CAT#:0804-HY-124593-03Size:10 mM - 1 mL
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH) . PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies[1][2].
CAS Number
1256565-36-2
Product Name Alternative
Emvododstat
UNSPSC
12352005
Target
Dihydroorotate Dehydrogenase; DNA/RNA Synthesis; VEGFR
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; Metabolic Enzyme/Protease; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/ptc299.html
Purity
99.89
Solubility
DMSO : 50 mg/mL (ultrasonic)
Smiles
O=C(N([C@H]1C2=CC=C(OC)C=C2)CCC3=C1NC4=C3C=C(Cl)C=C4)OC5=CC=C(Cl)C=C5
Molecular Formula
C25H20Cl2N2O3
Molecular Weight
467.34
References & Citations
[1]Cao L, et al. Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of DihydroorotateDehydrogenase with Favorable Pharmaceutical Properties. Mol Cancer Ther. 2019 Jan;18 (1) :3-16.|[2]Bender Ignacio RA, et al. Brief Report: A Phase 1b/Pharmacokinetic Trial of PTC299, a Novel PostTranscriptional VEGF Inhibitor, for AIDS-Related Kaposi's Sarcoma: AIDS Malignancy Consortium Trial 059. J Acquir Immune Defic Syndr. 2016 May 1;72 (1) :52-7.|[3]Zeng Z, et al, Targeting dihydroorotate dehydrogenase in acute myeloid leukemia. Haematologica. 2018 Sep;103 (9) :1415-1417.|[4]Packer RJ, et al. Phase I and pharmacokinetic trial of PTC299 in pediatric patients with refractory or recurrent central nervous system tumors: a PBTC study. J Neurooncol. 2015;121 (1) :217-224.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3

Chemical Information

Emvododstat

Emvododstat is an orally bioavailable, small molecule inhibitor of vascular endothelial growth factor (VEGF) synthesis with potential antiangiogenesis and antineoplastic activities. Emvododstat targets post-transcriptionally by selectively binding the 5'- and 3'-untranslated regions (UTR) of VEGF messenger RNA (mRNA), thereby preventing translation of VEGF. This inhibits VEGF protein production and decreases its levels in the tumor and bloodstream. In turn, this may result in the inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and eventually the induction of tumor cell death. VEGFs are upregulated in a variety of tumor cell types and play key roles during angiogenesis. In addition, emvododstat may enhance the antitumor activity of other chemotherapeutic agents.

CAS Number1256565-36-2
PubChem CID49787172
IUPAC Name(4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate
Molecular FormulaC25H20Cl2N2O3
Molecular Weight467.3
XLogP6.3
Topological Polar Surface Area54.6
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count3
Rotatable Bond Count4
Heavy Atom Count32
Formal Charge0
Complexity651
SMILES
COC1=CC=C(C=C1)[C@H]2C3=C(CCN2C(=O)OC4=CC=C(C=C4)Cl)C5=C(N3)C=CC(=C5)Cl
InChI
InChI=1S/C25H20Cl2N2O3/c1-31-18-7-2-15(3-8-18)24-23-20(21-14-17(27)6-11-22(21)28-23)12-13-29(24)25(30)32-19-9-4-16(26)5-10-19/h2-11,14,24,28H,12-13H2,1H3/t24-/m0/s1
InChIKey
SRSHBZRURUNOSM-DEOSSOPVSA-N
Chemical Structure
2D Structure
2D structure of Emvododstat
CAS: 1256565-36-2
CID: 49787172
Formula: C25H20Cl2N2O3
MW: 467.3
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight467.3
XLogP36.3
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count3
Rotatable Bond Count4
Exact Mass466.0850979
Monoisotopic Mass466.0850979
Topological Polar Surface Area54.6 Ų
Heavy Atom Count32
Formal Charge0
Complexity651
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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Alternative Products

CatalogName
BA3974-1PTC299
A18935-25PTC299 25mg
A18935-10PTC299 10mg
A18935-5PTC299 5mg
A18935-50PTC299 50mg
A18935-1PTC299 1mg
C01464-5mgEmvododstat (PTC299)
A18935-100PTC299 100mg
A18935-10mM-DPTC299 10mM * 1mL in DMSO

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