Perifosine（Akt inhibitor）

保质期 ：2 years

英文名 ：Perifosine（Akt inhibitor）

库存 ：10

供应商 ：上海伟进生物科技有限公司

CAS号 ：157716-52-4

保存条件 ：-20℃

规格 ：5mg

Biological Activity

Perifosine is a novel synthetic alkylphospholipid (ALP) ^[1], a new class of antitumor agent which targets cell membranes, inhibits Akt activation and induces apoptosis in PC-3 prostate carcinoma cells ^[2], epithelial carcinoma cell line A431 as well as HeLa cells^[3]. The structure of perifosine is similar to naturally-occurring phospholipids. Perifosine (5 μM) causes growth inhibition of PC-3 cells by 50% (GI₅₀) in 24 h and induces virtually all cells to die by 48 h. Perifosine also inhibits the growth of other cell types, with GI₅₀ values of 1-10 µM [K-562, SUDHL-7, HL-60, PC-3, Colo-205, and MESA-SA (CRL-1976)], 11-30 µM [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], and >30 µM [MCF-7, Hos (CRL-1543), and LnCAP]. Perifosine does not directly affect activity of PI3-K or phosphoinositide-dependent kinase 1. It reduces Akt activity by inhibiting phosphorylation of Akt at both Thr308 and Ser473 ^[3]. Combination treatment with perifosine and HDACIs in human leukemia cells inhibits both Akt and MEK/ERK, increases ceramide and ROS production, and strikingly increases mitochondrial injury and apoptosis ^[4]. Perifosine, a novel oral bioactive ALP, displays significant antiproliferative activity in vitro and in vivo in several human tumor model systems and is currently being tested in different stages of clinical trials, especially phase 3 trials for colorectal cancer and multiple myeloma ^[5-7].

Chemical Properties

Cas No.: 157716-52-4	M. Wt.: 461.66
Formula: C25H52NO4P	Purity: >99%
Synonym: KRX-0401, NKA17, D-21266, NSC 639966
Chemical Name: Octadecyl-(1,1-dimethyl-4-piperidylio)phosphate
Appearance: White to off-white solid
Solubility: Soluble in ethanol at 30 mg/mL, soluble in water at 10 mg/mL with warming. Poorly soluble in DMSO.
Storage：Store solid at -20 ºC for the stability up to two years.