N3PT
N3PT Basic information
- Product Name:
- N3PT
- Synonyms:
-
- N3PT
- N3-pyridyl thiaMine
- 3-[(2-Amino-6-methyl-3-pyridyl)methyl]-5-(2-hydroxyethyl)-4-methylthiazolium chloride hydrochloride
- N3PT,N-3PT
- 3-((2-Amino-6-methylpyridin-3-yl)methyl)-5-(2-hydroxyethyl)-4-methylthiazol-3-ium chloride hydrochloride
- CID 66970987
- CAS:
- 13860-66-7
- MF:
- C13H19Cl2N3OS
- MW:
- 336.28046
- Mol File:
- 13860-66-7.mol
N3PT Chemical Properties
- Melting point:
- 225℃
- storage temp.
- Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
- solubility
- DMSO : 2.86 mg/mL (8.50 mM; Need ultrasonic)
- form
- Powder
- color
- Light yellow to yellow
N3PT Usage And Synthesis
Uses
N3PT (N3-pyridyl thiamine) is a potent and selective transketolase inhibitor. N3PT is pyrophosphorylated and then binds to transketolase with an Kd value of 22 nM (Apo-TK, transketolase lacking bound thiamine)[1].
in vivo
N3PT (compound 1) (100 mg/kg; i.v.; twice a day; 2 weeks) shows inhibitory effect on transketolase activity without significantly anti-tumor activity in HCT-116 tumor-bearing nude mice[1].
| Animal Model: | HCT-116 tumor-bearing nude mice[1] |
| Dosage: | 100 mg/kg |
| Administration: | Intravenous injection; twice a day; 2 weeks |
| Result: | Decreased the activity of transketolase with no apparent effect on tumor size. Indicated that there were alternative pathways to generate ribose for DNA synthesis that were operating in these tumor cell lines. |
References
[1] Thomas AA, et al. Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2206-10. DOI:10.1016/j.bmcl.2007.11.101
[2] Jeno Gyuris, May Han, Ronan C, N3-pyridyl-thiamine and its use in cancer treatments. Patent Numeber: WO2005094803 A2
[3] Allen A. Thomas, Josh Ballard, Bryan Bernat. Potent and Selective Thiamine Antagonists
That Inhibit Transketolase.
[4] Thomas AA, De Meese J, Le Huerou Y, Non-charged thiamine analogs as inhibitors of enzyme transketolase. Bioorg Med Chem Lett. 2008 Jan 15;18(2):509-12. DOI:10.1016/j.bmcl.2007.11.098
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