米替福新 - CAS:58066-85-6 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	米替福新热销
英文名称:	Miltefosine
别名:	米替福新 HePC Hexadecyl phosphocholine
CAS No:	58066-85-6	分子式:	C₂₁H₄₆NO₄P	分子量:	407.57
CAS No:	58066-85-6
分子式:	C₂₁H₄₆NO₄P
分子量:	407.57
MDL:	MFCD00133396

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M60007 米替福新 ≥98% (psaitong)

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熔点：

232.2-233.9°C

包装规格：

500mg 1g 5g in glass bottle

溶解性：

溶于水(10mg/ml)、DMSO(800μg/ml)、乙醇(1mg/ml)

产品描述：

基本信息

产品编号：	M60007
产品名称：	Miltefosine
CAS:	58066-85-6	储存条件	粉末	-20℃	四年

分子式：	C21H46NO4P		溶于液体	-80℃	6个月
分子量：	407.57			-20℃	1个月
化学名：	HePC Hexadecyl phosphocholine
Solubility (25°C)：
体外:	DMSO	Insoluble
	Ethanol	81mg/mL (198.73mM)
	Water	81mg/mL (198.73mM)
体内(现配现用):	Saline	30mg/mL
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.4536mL	12.2678mL	24.5357mL
5mM	0.4907mL	2.4536mL	4.9071mL
10mM	0.2454mL	1.2268mL	2.4536mL

生物活性

产品描述	一种诱导组胺释放的PI-3/Akt抑制剂，ED50分别为17.2μM和8.1μM。
靶点	Akt;HIV-1
体外研究	Treatment of HIV-1 infected macrophages with Miltefosine inhibits the recruitment of PH-AktGFP to the plasma membrane.Since Miltefosine inhibits Akt through mimicry of the PH domain,it is likely that Miltefosine binds to PIP3,blocking the recruitment of PH-Akt to the membrane.Miltefosine (HePC) inhibits protein kinase C (PKC) from NIH3T3 cells in cell-free extracts with a IC50 of about 7µM.Inhibition is competitive with regard to phosphatidylserine with a Ki of 0.59µM.Miltefosine is an alkylphospholipid that inhibit activation of Akt.Miltefosine is a direct inhibitor of Akt,and induces dosedependent inhibition of primary effusion lymphoma (PEL) in culture and also inhibits the downstream targets of Akt,such as mTOR,leading to reduced phosphorylation and activation of S6K and S6.Importantly,Miltefosine also inhibits Akt targets that are not part of the mTOR pathway,eg,FOXO1,and are therefore expected to have a greater therapeutic impact than mTORC1 inhibitors alone.
体内研究	Mice are randomized into groups of 5 and injected intraperitoneally 5 days a week with 50mg/kg of either Miltefosine or Perifosine dissolved in PBS,or equivalent volume of vehicle (PBS).Both Miltefosine and Perifosine inhibit the growth rate of tumors compared with vehicle-treated mice.By day 14 after treatment,there is an approximately 50% decrease in average tumor volume in Perifosine-and Miltefosine-treated mice,compared with vehicle-treated mice (P<0.04).Tumor growth is also significantly retarded (P<0.04 for Perifosine and P≤0.055 for Miltefosine by linear mixed-effects model analysis).Immunohistochemical analyses display an overall reduction in staining for phosphorylated ribosomal S6 protein in tumor sections from Miltefosine- and Perifosine-treated mice compared with the PBS-treated mice.This reduced phosphorylation correlated with the delay in tumor progression in drug-treated animals.

推荐实验方法(仅供参考)

激酶实验：

Levels of enzymatically active caspase-3 are quantified using the ApoAlert Caspase Fluorescent assay kit.Briefly,1×106 BC-1 PEL cells are treated with 50μM Miltefosine,50μM Perifosine,or 20nM NVP-BEZ235,as well as the respective vehicle controls.Cells are harvested and lysed 12 hours later.Equivalent micrograms of cell lysate for all samples are incubated with a fluorogenic caspase-3 substrate (DEVD-AFC).Cleavage of DEVD by caspase-3 releases AFC,the fluorescence of which is measured using a FLUOstar OPTIMA fluorometer,with excitation and emission filter wavelengths set to 400 and 505nm,respectively.

细胞实验:

NIH3T3 cells are grown in DMEM supplemented with 10% FCS in a humidified atmosphere of 95% air with 5% CO2.Cells are plated on 35-mm culture dishes (6-well plates) at 0.5-0.8×105 cells/well.Growth is established for 18-24h and the cell number of representative wells is determined (time 0).The experiments are started by addition of fresh prepared solution of Miltefosine at given concentrations to the cells or equal volumes of Tris-HCI to control cells.After incubation for 60h,cells are counted with an electronic counter.Cellular multiplication is calculated.

动物实验:

Mice

PEL cells are washed in ice-cold phosphate buffered saline, counted,and diluted in 100μL of PBS mixed with 100μL of growth factor-depleted Matrigel.A total of 1×105 to 7.5×105 BC-1 cells are injected subcutaneously into the right flank of NOD.CB17-Prkdcscid/J or CB17-Prkdcscid/J mice.The mice are monitored on alternate days for development of palpable tumors (2 mm3),at which point drug or vehicle treatments are initiated,and are administered either intraperitoneally (Perifosine) or by oral gavage (Rosiglitazone,NVP-BEZ235) 5 days a week.Groups of 5 to 7 mice are used to generate PEL tumors and treated with either vehicle or drug cocktail.Each biologic experiment is repeated multiple times.For Rosiglitazone,0.25% methylcellulose is used as vehicle,and 30mg/kg or 60mg/kg Rosiglitazone is suspended in methylcellulose.For Perifosine and Miltefosine,PBS is used as a vehicle and 50mg/kg Perifosine or Miltefosine is dissolved in PBS.For NVP-BEZ235,the compound is dissolved in a 1:9 vol/vol mixture of 1-methyl-2-pyrrolidone and polyethylene glycol 300.A dose of 40mg/kg NVP-BEZ235 or equal volume of the vehicle is administered.Tumor diameters are measured using digital calipers,and tumor volume is calculated.The tumors are excised and fixed in formalin.Statistical analyses are performed using linear model fit by maximum likelihood with individual animals treated as random effect.

Rats

Male Sprague-Dawley rats (weight 270-290g) are divided into five groups (n=5).Rats in the treatment groups are administered a single 10mg/kg oral dose of Miltefosine (MFS) either as an aqueous solution or MFS-LNCs dispersion by gastric gavage.This dose is equivalent to the 20mg/kg Miltefosine dose administered to mice in the preclinical study after correction for rats.Following administration,blood samples are collected via the orbital plexus under anesthesia at time intervals of 0.5,1,2,4,7,10,24,48,72 and 216h in Eppendorf tubes containing EDTA.Blood samples are then centrifuged immediately at 4000 rpm for 10 min.Plasma samples are frozen and maintained at -80℃ pending analysis.

保存条件：

-20℃

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