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- 文献和实验
- 技术资料
- 保存条件：
见说明书
- 保质期：
＞1年
- 英文名：
Perifosine
- 库存：
期货2-3周
- 供应商：
上海经科化学科技有限公司
- CAS号：
157716-52-4
- 规格：
5mg
供应商：上海经科化学科技有限公司
服务热线：400-0199-638
QQ:472482400(上海经科）
微信号：shjkchem
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本试剂(Perifosine)
仅供科研实验使用,不得用于其他用途！
货 号：P-6522
名 称：Perifosine
别 名：Perifosine
C A S ：157716-52-4
分子量：461.66
分子式：C25H52NO4P
纯 度：HPLC/TLC:>99%
说 明：Storage: Store at or below -20 ºC. Solubility: Very poorly soluble in DMSO; soluble in ethanol at 200 mg/mL; soluble in water at 50 mg/mL with warming; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.
文 献：The structure of perifosine is similar to naturally-occurring phospholipids. Perifosine (5 µM) inhibited the growth of PC-3 prostate carcinoma cells by 50% in 24 hr and induced cell death in virtually all cells by 48 hr. Kondapaka, S.B., et al. "Perifosine, a novel alkylphospholipid, inhibits protein kinase B activation." Mol. Cancer Ther. 2: 1093-1103 (2003). Perifosine inhibits the growth of variant cells, with GI50 values of 1-10 µM for K-562, SUDHL-7, HL-60, PC-3, Colo-205, and MESA-SA (CRL-1976) cells, 11-30 µM for MG-63 (CRL-1427), H-3386, RD (CCL-136), HT-29, MDA-435, SW-620, CCRF-7, H-1355, SAJA-1 (CRL-2098), and DU-145 cells, and >30 µM for MCF-7, Hos (CRL-1543), and LnCAP cells. Kondapaka, S.B., et al. "Perifosine, a novel alkylphospholipid, inhibits protein kinase B activation." Mol. Cancer Ther. 2: 1093-1103 (2003). Perifosine reduces Akt activity by inhibiting phosphorylation of Akt at both Thr308 and Ser473. Kondapaka, S.B., et al. Perifosine, a novel alkylphospholipid, inhibits protein kinase B activation." Mol. Cancer Ther. 2: 1093-1103 (2003). Perifosine inhibited the growth of breast, ovarian and prostate cancers by inducing apoptosis. Perifosine selectively blocks AKT recruitment to the membrane and down-regulates the phosphorylation of AKT and its downstream targets, particularly S6, in various tumor cell lines and xenografts. Hennessy, B.T., et al. "Pharmacodynamic markers of perifosine efficacy." Clin. Cancer Res. 13: 7421-7431 (2007). Perifosine induces significant in vitro and in vivo cytotoxicity in human multiple myeloma (MM), which is associated with down-regulation of Akt phosphorylation in tumor cells. c-Jun N-terminal kinase (JNK) plays a critical role in perifosine-induced apoptosis. Perifosine enhances dexamethasone, doxorubicin, melphalan and bortezomib-induced MM cell cytotoxicity. Hideshima, T., et al. "Perifosine, an oral bioactive novel alkylphospholipid, inhibits Akt and induces in vitro and in vivo cytotoxicity in human multiple myeloma cells." Blood 107: 4053-4062 (2006). No significant clinical activity of perifosine against androgen independent prostate cancer was observed in a phase II study. Posadas, E.M., et al. "A phase II study of perifosine in androgen independent prostate cancer." Cancer Biol. Ther. 4: 1133-1137 (2005). Twenty-three patients with advanced soft tissue sarcoma received 66 cycles of treatment with perifosine (1 cycle = 4 weeks). The 3 and 6 month progression-free survival was 22% and 9%. Bailey, H.H., et al. "Phase II study of daily oral perifosine in patients with advanced soft tissue sarcoma." Cancer 107: 2462-2467 (2006).
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文献和实验相关实验
Institute. Perifosine：A p.o.-bioavailable ALK(Alkylphospholipids),inhibits Akt activation。 AT7867 is a potent and oral AKT and p70 S6 kinase inhibitor with an IC50 of 17 nM. GSK690693：selective for the Akt isoforms(inhibits Akt
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Perifosine
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