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. |