PTC299 (Synonyms: PTC-299) |
| Catalog No.GC65335 |
PTC299 est un inhibiteur actif par voie orale de la traduction de l'ARNm du VEGFA qui inhibe sélectivement la synthèse de la protéine VEGF au niveau post-transcriptionnel. PTC299 est également un puissant inhibiteur de la dihydroorotate déshydrogénase (DHODH). PTC299 montre une bonne biodisponibilité orale et une absence d'inhibition de la kinase hors cible et de myélosuppression. PTC299 peut être utile pour la recherche d'hémopathies malignes.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1256565-36-2
Sample solution is provided at 25 µL, 10mM.
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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].
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 A 77-1726 in leukemia cells[1].
[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]. 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.
[4]. Zeng Z, et al, Targeting dihydroorotate dehydrogenase in acute myeloid leukemia. Haematologica. 2018 Sep;103(9):1415-1417.
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