Other drug agents
MedKoo product information:
Description of Kevetrin: Kevetrin (thioureidobutyronitrile), is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity. Upon intravenous administration, thioureidobutyronitrile activates p53 which in turn induces the expressions of p21 and PUMA (p53 up-regulated modulator of apoptosis), thereby inhibiting cancer cell growth and causing tumor cell apoptosis. Thioureidobutyronitrile may be effective in drug-resistant cancers with mutated p53. p53 tumor suppressor, a transcription factor regulating the expression of many stress response genes and mediating various anti-proliferative processes, is often mutated in cancer cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). (last updated: 9/2/2015).
Current developer: Cellceutix / Formatech
Note: The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Protocols from literature
Kevetrin is currently being developed by Cellceutix, who reported a recent study on Kevetrin™. The results show that Kevetrin has potent antitumor activity in several wild type and mutant p53 human tumor xenografts e.g. A549, PC-3, MDA-MB-231, HT-29, NCI-H1975, HCT-15, K-562, LNCaP. Kevetrin is non-genotoxic. DNA damaging drugs result in rapid phosphorylation of H2A.X at Ser 139 by PI3K-like kinases; however, Kevetrin did not induce phosphorylation of H2A.X. Since Kevetrin was well-tolerated in GLP safety pharmacology and toxicity studies. (source: http://cancerres.aacrjournals.org/cgi/content/short/72/8_MeetingAbstracts/2874?rss=1).
1. Nitrile derivatives and their pharmaceutical use
and compositions By Menon, Krishna
(Keyword; CAS#; MedKoo Cat#)
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