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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EMD Millipore
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United States
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25 May 2012
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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.
| Product information | |||
|---|---|---|---|
| Form | White solid | ||
| Primary Target | PFTase | ||
| Primary Target IC50 | 530 nM (mammalian) | ||
| Secondary target | protein geranylgeranyltransferase-I (IC50 > 10 µM for mammalian) | ||
| Molar mass | 542.7 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Cell permeable | Yes | ||
| Purity | ≥95% by HPLC | ||
| Solubility | DMSO or MeOH | ||
| Chemical formula | C31H34N4O3S | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Shipped with Blue Ice or with Dry Ice
Standard Handling |
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