Perifosine **
產品名稱：Perifosine
產品貨號：LC P-6522
產品規(guī)格：100 MG
Perifosine, also known as KRX-0401, is a novel synthetic alkylphospholipid and is a new kind of antitumor agent which targets cell membranes and blocks Akt activation.
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).
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
