344559
FTI-2628
2-(((5-((1H-Imidazol-4-ylmethyl)-amino)-methyl)-2′-methyl-biphenyl-2-carbonyl)-amino)-4-methylsulfanyl-butyric acid benzyl ester
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メルク株式会社
目黒区下目黒1-8-1
153-8927 東京
Japan
TEL： 0120-189-390
Fax: 0120-189-350
E-mail mj_service@merckgroup.com
31 5月 2012
ローディング
A cell-permeable benzyl ester prodrug form of FTI-2148 (Cat. No. 344557) that preferentially inhibits protein farnesyltransferase activity (IC50 = 530 nM for mammalian and 1.0 µM for P. falciparum) over protein geranylgeranyltransferase-I (IC50 > 10 µM for mammalian) and displays anti-malarial properties. Potently disrupts Ras farnesylation in H-Ras-transformed NIH 3T3 cells (IC50 = 20 nM) and inhibits the growth of P. falciparum in red blood cells (ED50 = 150 nM). Also suppresses parasitemia in P. berghei-infected mice by 46.1% (50 mg/kg, ip) with no apparent toxicity.
| 製品情報 | |||
|---|---|---|---|
| Form | White solid | ||
| Primary Target | PFTase | ||
| Primary Target IC50 | 530 nM (mammalian) | ||
| Secondary target | protein geranylgeranyltransferase-I (IC50 > 10 µM for mammalian) | ||
| Protect from Light | はい | ||
| Packaged under inert gas | はい | ||
| Cell permeable | はい | ||
| Purity | ≥95% by HPLC | ||
| 化学式 | C31H34N4O3S | ||
| 保管と送付情報 | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Shipped with Blue Ice or with Dry Ice
Standard Handling |
||
