Acivicin hợp chất kháng MIA PaCa-2 (tế bào gây ung thư tụy)
From Wikipedia, the free encyclopedia
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| Names | |
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| IUPAC name
(2S)-Amino[(5S)-3-chloro-4,5-dihydro-1,2-oxazol-5-yl]ethanoic acid
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| Other names
Antibiotic AT 125
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| Identifiers | |
3D model (JSmol)
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| ChEBI | |
| ChemSpider | |
PubChem CID
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| UNII | |
| Properties | |
| C5H7ClN2O3 | |
| Molar mass | 178.574 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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 verify (what is   ?) | |
| Infobox references | |
It is a fermentation product of Streptomyces sviceus.[1] It interferes with glutamate metabolism and inhibits glutamate dependent synthesis of enzymes, and is thereby potentially helpful in treatment of solid tumors.[2]
After its discovery in 1972, acivicin was studied as an anti-cancer agent, but trials were unsuccessful due to toxicity.[3]
Contents
[hide]Research[edit]
An in vitro study showed that Acivicin at a concentration of 5 µM Acivicin inhibited by 78% the growth of human pancreaticcarcinoma cells (MIA PaCa-2) after 72 hours in continuous culture. It was also found that acivicin at a concentration of 450 µM irreversibly inactivated MIA PaCa-2 γ-glutamyl transpeptidase (10 nmol/min/106 cells) with an inactivation half-life of 80 minutes.[1]
Phase I studies[edit]
Phase I dose escalating studies conducted in 23 cancer patients administered acivicin with a concomitant 96-h i.v. infusion of a mixture of 16 amino acids showed reversible, dose-limiting CNS toxicity, characterized by lethargy, confusion and decreased mental status.
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