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PTC299

  Cat. No.:  DC12482   Featured
Chemical Structure
1256565-36-2
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More than 5000 active chemicals with high quality for research!
Field of application
PTC299 (PTC-299) is a novel potent inhibitor of dihydroorotate dehydrogenase (DHODH), inhibits hypoxia-induced VEGFA protein production in HeLa cells with IC50 of 1.64 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1256565-36-2
Chemical Name: 4-chlorophenyl (S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indole-2-carboxylate
Synonyms: PTC-299;PTC 299
SMILES: N1C2=C(CCN([C@@H]2C2C=CC(OC)=CC=2)C(=O)OC2C=CC(Cl)=CC=2)C2C=C(C=CC1=2)Cl
Formula: C25H20Cl2N2O3
M.Wt: 467.34
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1. Cao L, et al. Mol Cancer Ther. 2018 Oct 23. pii: molcanther.0863.2018.
Description: PTC299 is a dihydroorotate dehydrogenase (DHODH) inhibitor, has broad and potent activity against hematological cancer cells[1]. PTC299, also an orally bioavailable VEGF inhibitor, acts through posttranscriptional regulation of VEGF mRNA under conditions of cellular stress[2].
Target: Dihydroorotate dehydrogenase[1], VEGF[2]
In Vitro: PTC299 inhibits hypoxia-induced VEGFA protein production in HeLa cells with an EC50 of 1.64 ± 0.83 nM[1]. PTC299 is the most potent inhibitor with an IC50 of about 1 nM, over 10 to 1000-fold more potent than Brequinar, Vidofludimus or Teriflunomide in leukemia cells[1].
References: [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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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