Reparixin L-lysine salt

Perifosine is an orally active alkyl phospholipid analogue that has shown antitumor activity in a variety of cancers by interfering .

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库存: 现货

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5mg

￥1087.00

870.00

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10mg

￥2987.00

2390.00

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￥5937.00

4750.00

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50mg

￥9175.00

7340.00

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货号: ajci11868
CAS: 266359-93-7
别名: REPERTAXINL-赖氨酸盐,Repertaxin L-lysine salt
分子式: C20H35N3O5S
分子量: 429.57
纯度: >98%
溶解度: ≥ 21.5 mg/mL in DMSO, ≥ 66.67 mg/mL in EtOH, ≥ 16.67 mg/mL in Water with gentle warming
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.

Protocol

Cell experiment [1]:
Cell lines
Preparation Method	Cells were incubated with increasing concentrations of perifosine for 24h, 48h and 72h and the number of viable cells was determined by crystal violet staining.
Reaction Conditions	10μM-40μM;24h, 48h and 72h
Applications	AKT phosphorylation was dose-dependently inhibited by perifosine. Concomitantly, perifosine displayed anti-tumor activity in both cell lines.
Animal experiment [2]:
Animal models	Five-week-old male BALB/c nude mice
Preparation Method	DU 145 or H1915 cells were subcutaneously inoculated into the right flank of mice and allowed to form a palpable tumor.
Dosage form	45 and 180 mg/kg;p.o
Applications	Perifosine Preferably Accumulates in H1915 Tumor Xenografts. Perifosine Reduced Cell Proliferation and Induced Apoptosis Preferentially in H1915 Tumor Xenografts.
参考文献: [1]. 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. [2]. 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.