Reparixin L-lysine salt (Synonyms: Repertaxin) |
| Catalog No.GC13813 |
Perifosine is an orally active alkyl phospholipid analogue that has shown antitumor activity in a variety of cancers by interfering .
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Cas No.: 266359-93-7
Sample solution is provided at 25 µL, 10mM.
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Perifosine is an orally active alkyl phospholipid analogue that has shown antitumor activity in a variety of cancers by interfering with Akt membrane translocation targeting Akt activity and inhibiting AKT phosphorylation[1-3].
Perifosine (0.5 µM) blocked Akt activation in all three pancreatic cancer cell lines(PANC-1, MIA and AsPC-1)[6]. AKT phosphorylation was dose-dependently inhibited by perifosine(10µM-40µM;24h, 48h and 72h). Concomitantly, perifosine displayed anti-tumor activity in both cell lines[4].
Perifosine(45 and 180 mg/kg;p.o) Accumulates in H1915 Tumor Xenografts. Perifosine Reduced Cell Proliferation and Induced Apoptosis Preferentially in H1915 Tumor Xenografts[5]. In vivo, perifosine (1 mg/kg; i.g;once daily for 20 days) and ABT-737 co-administration strikingly inhibited A549 lung cancer xenograft growth in nude mice[7].
References:
[1]. Holohan B, Hagiopian MM, et,al Perifosine as a potential novel anti-telomerase therapy. Oncotarget. 2015 Sep 8;6(26):21816-26. doi: 10.18632/oncotarget.5200. PMID: 26307677; PMCID: PMC4673128.
[2]. Fensterle J, Aicher B, et,al. Current view on the mechanism of action of perifosine in cancer. Anticancer Agents Med Chem. 2014 May;14(4):629-35. doi: 10.2174/1871520614666140309225912. PMID: 24628236.
[3]. Chen MB, Wu XY, et,al. Perifosine sensitizes curcumin-induced anti-colorectal cancer effects by targeting multiple signaling pathways both in vivo and in vitro. Int J Cancer. 2012 Dec 1;131(11):2487-98. doi: 10.1002/ijc.27548. Epub 2012 Jul 3. PMID: 22438101.
[4]. Engel JB, Honig A, et,al. Perifosine inhibits growth of human experimental endometrial cancers by blockade of AKT phosphorylation. Eur J Obstet Gynecol Reprod Biol. 2008 Nov;141(1):64-9. doi: 10.1016/j.ejogrb.2008.06.007. Epub 2008 Aug 6. PMID: 18687514.
[5]. Taniguchi K, Suzuki T, et,al. Perifosine, a Bioavailable Alkylphospholipid Akt Inhibitor, Exhibits Antitumor Activity in Murine Models of Cancer Brain Metastasis Through Favorable Tumor Exposure. Front Oncol. 2021 Nov 4;11:754365. doi: 10.3389/fonc.2021.754365. PMID: 34804943; PMCID: PMC8600181.
[6]. Xin Y, Shen XD, et,al. Perifosine inhibits S6K1-Gli1 signaling and enhances gemcitabine-induced anti-pancreatic cancer efficiency. Cancer Chemother Pharmacol. 2014 Apr;73(4):711-9. doi: 10.1007/s00280-014-2397-9. Epub 2014 Feb 12. PMID: 24519751.
[7]. Shen J, Xu L, et,al. Perifosine and ABT-737 synergistically inhibit lung cancer cells in vitro and in vivo. Biochem Biophys Res Commun. 2016 May 13;473(4):1170-1176. doi: 10.1016/j.bbrc.2016.04.035. Epub 2016 Apr 9. PMID: 27073162.
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