For the science "geeks" on the board: Kevetrin
Post# of 72440
For the science "geeks" on the board:
Kevetrin
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 ).
Current developer: Cellceutix
| MedKoo Code#: 205891 | |
| Name: Kevetrin | |
| CAS#: 66592-89-0 (Kevetrin HCl); 500863-50-3 (Kevetrin) Synonym: Kevetrin; thioureidobutyronitrile; thioureido butyronitrile IUPAC/Chemical name: 3-cyanopropyl carbamimidothioate hydrochloride | |
| Chemical structure | Theoretical analysis |
| | Kevetrin HCl salt Chemical Formula: C5H10ClN3S Kevetrin (free base) Chemical Formula: C5H9N3S |
| Availability and price: This agent is not in stock, which may be available through custom synthesis. To inquire quotation and lead time or to ask questions, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.
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| Highlights of recent research using this agent |
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...2874?rss=1 ).
| References |
1. Nitrile derivatives and their pharmaceutical use and compositions By Menon, Krishna
From U.S. Pat. Appl. Publ. (2012), US 20120189537 A1 20120726.
2. Nitrile derivatives and their pharmaceutical use and compositions By Menon, Krishna
From PCT Int. Appl. (2010), WO 2010135170 A2 20101125.
3. Preparation of 4-isothioureido butyronitrile hydrochloride derivatives for treatment of cancer By He, Lan; Pan, Xuan From Faming Zhuanli Shenqing (2009), CN 101550098 A 20091007.
4. Preparation of protein conjugates via intermolecular disulfide bond formation By King, Te Piao; Li, Yen; Kochoumian, Loucia From Biochemistry (1978), 17(8), 1499-506.
5. Preparation of some amino sulfonamides By Miller, Ellis; Sprague, James M.; Kissinger, L. W.; McBurney, Lane F. From Journal of the American Chemical Society (1940), 62, 2099-102.
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