PTC299

SKU: orb1309211

Description

PTC299 is an orally bioavailable small molecule that selectively inhibits VEGFA protein synthesis post-transcriptionally and potently targets dihydroorotate dehydrogenase (DHODH). It has been investigated in preclinical in vitro and in vivo studies for its potential application in angiogenesis-dependent research areas, including oncology.

Research Area

Cardiovascular Research, Cell Biology, Metabolism Research, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 1256565-36-2
• MW: 467.34
• Purity: 99.19% (May vary between batches)
• Formula: C₂₅H₂₀Cl₂N₂O₃
• SMILES: COc1ccc(cc1)[C@@H]1N(CCc2c1[nH]c1ccc(Cl)cc21)C(=O)Oc1ccc(Cl)cc1
• Target: VEGFR|||Dehydrogenase
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (2.14 mM);DMSO:50 mg/mL (106.99 mM)

Bioactivity

• In Vitro:
  PTC299 as an inhibitor of VEGFA mRNA translation in a phenotypic screen and evaluated in the clinic for treatment of solid tumors. To guide precision cancer treatment, we performed extensive biological characterization of the activity of PTC299 and demonstrated that inhibition of VEGF production and cell proliferation by PTC299 is linked to a decrease in uridine nucleotides by targeting dihydroorotate dehydrogenase (DHODH), a rate-limiting enzyme for de novo pyrimidine nucleotide synthesis.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dihydroorotate Dehydrogenase, DHODH, DNA/RNA Synthesis, cancer, (4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate, oral, off-target, kinase, inhibit, myelosuppression, malignancies, hematologic, Inhibitor, Emvododstat, PTC299, PTC-299, PTC 299, Vascular endothelial growth factor receptor, VEGFR

Compound Identifiers

PubChem CID

49787172