Detail of "157716-52-4"

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Phase II study of daily oral perifosine in patients with advanced soft tissue sarcoma

All Rights Reserved. Phase II study of daily oral perifosine in patients with advanced soft tissue sarcoma. Bailey, Howard H.; Mahoney, Michelle R.; Ettinger, David S.; Maples, William J.; Fracasso, Paula M.; Traynor, Anne M.; Erlichman, Charles; Okuno, Scott H. (University of Wisconsin Comprehensive Cancer Center, Madison, WI, USA). Cancer (Hoboken, NJ, United States), 107(10), 2462-2467 (English) 2006 John Wiley & Sons, Inc. CODEN: CANCAR. ISSN: 0008-543X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Backround: A multicenter Phase II study was performed to evaluate the clin. activity of an initial loading (150 mg every 6 h ′ 4 doses) dose followed by continuous daily oral dosing (100 mg/day) of perifosine in patients with advanced soft tissue sarcomas (STSs). 157716-52-4 which is the cas registry number is also used here. Methods: Patients with measurable metastatic STS received perifosine as first-, second-, or third-line treatment and underwent disease assessment every 8 wk until disease progression, excessive toxicity, or patient refusal. Results: Twenty-three patients received 66 cycles (1 cycle = 4 wk) of perifosine. One partial response of 9 mo duration was obsd. The overall 3 and 6 mo progression-free survival was 22% and 9%. NCI CTC (v2.0) Grade 1 to 2 gastrointestinal toxicity or fatigue were the most common (>50% of subjects) toxicities obsd. The steady-state plasma perifosine levels (Css) were similar to prior experience (mean 6 mg/mL). Patients with Css levels >6 mg/mL appeared more likely to remain on study past 2 mo than those with levels <6 mg/mL. Conclusions: Despite not achieving the primary objective of 340% 6-mo progression-free survival rate, optimism remains for this agent in STS patients. Prolonged responses in heavily pretreated STS patients continue to be obsd. with perifosine treatment. Continued assessment of perifosine in STS appears warranted, with special attention to specific histologies or tumor characteristics that might identify a more sensitive population and achieving perifosine Css levels >6 mg/mL. .

Spin-Labeled Alkylphospholipids in a Dipalmitoylphosphatidylcholine Bilayer: Molecular Dynamics Simulations

All Rights Reserved. Spin-Labeled Alkylphospholipids in a Dipalmitoylphosphatidylcholine Bilayer: Molecular Dynamics Simulations. Mravljak, Janez; Konc, Janez; Hodoscek, Milan; Solmajer, Tom; Pecar, Slavko (Faculty of Pharmacy, University of Ljubljana, Ljubljana SI-1000, Slovenia). Journal of Physical Chemistry B, 110(51), 25559-25561 (English) 2006 American Chemical Society. CODEN: JPCBFK. ISSN: 1520-6106. DOCUMENT TYPE: Journal CA Section: 6 (General Biochemistry) Mol. dynamics simulation has been performed to investigate the structural properties of perifosine and its synthetic spin-labeled alkylphospholipid analogs. The conformations adopted by these compds. in water and in a dipalmitoylphosphatidylcholine bilayer as a function of the presence and position of the N-oxyl-4',4'-dimethyloxazolidine ring (doxyl group) have been investigated by all-atom mol. dynamics. No predominant conformation was obsd. in water, but the mols. adopt specific orientations and conformations in the lipid bilayer. 922174-82-1 and 157716-52-4 are cas registry numbers of chemicals which are used as reagents here. As is expected, alkyl chains tend to insert into the hydrophobic core, while charged groups stay at the lipid-water interface. A doxyl group in the middle of the alkyl chain moves up to the interface region, thus preventing adoption of the extended conformation. Compds. with a doxyl group close to the polar head group adopt conformations similar to that of unlabeled perifosine within the first nanoseconds of simulation. When the doxyl group is at the end of alkyl chain, the spin-labeled mol. needs more time to reach equil. These results indicate a considerable effect of the doxyl position within the alkyl chain on its localization in the lipid bilayer and can be extended further to other similar spin probes used in the ESR spectroscopy of biol. membranes. .