PTC299

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].

Product Specifications

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.