Perifosine

别名: KRX-0401, NSC639966, D21266 中文名称:哌立福新

Perifosine是一种新型的Akt抑制剂,在MM.1S细胞中IC50为4.7 μM,靶向作用于Akt的pleckstrin同源结构域。Phase 3。

Perifosine Chemical Structure

Perifosine Chemical Structure

CAS: 157716-52-4

规格 价格 库存 购买数量
5mg 1220.79 现货
25mg 3849.3 现货
50mg 7117.44 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

免费分装
免费预溶

Perifosine相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
NCI-H727 Cell Viability Assay 0-100 μM 24/72 h decreases cell viability in both dose and time dependent manner 22499437
GOT1 Cell Viability Assay 0-100 μM 24/72 h decreases cell viability in both dose and time dependent manner 22499437
BON1 Cell Viability Assay 0-100 μM 24/72 h decreases cell viability in both dose and time dependent manner 22499437
BON1 Apoptosis Asssay 0-10 μM 24 h induces apoptosis dose dependently 22499437
BON1 Function Assay 7.5/10 μM 8 h decreases the expression of the anti-apoptotic proteins BCL2 and Bcl-XL 22499437
Kasumi-1 Cell Viability Assay 0-20 μM 24/48 h decreases cell viability in both dose and time dependent manner 22407228
HL-60 Cell Viability Assay 0-20 μM 24/48 h decreases cell viability in both dose and time dependent manner 22407228
Kasumi-1 Apoptosis Asssay 10 μM 24 h induces apoptosis 22407228
HL-60 Apoptosis Asssay 10 μM 24 h induces apoptosis 22407228
Kasumi-1 Function Assay 2.5/5/10 μM 24 h decreases Akt and p-Akt levels dose-dependently 22407228
HL-60 Function Assay 2.5/5/10 μM 24 h decreases Akt and p-Akt levels dose-dependently 22407228
Kasumi-1 Function Assay 2.5/5/10 μM 24 h induces the phosphorylation of JNK1/2 in a dose dependent manner 22407228
HL-60 Function Assay 2.5/5/10 μM 24 h induces the phosphorylation of JNK1/2 in a dose dependent manner 22407228
K562 Function Assay 20 μM 48 h induces autophagy  22407228
OCUT1 Growth Inhibition Assay 0.1-3 μM 5 d inhibits cell growth in a dose dependent manner 22090271
K1 Growth Inhibition Assay 0.1-3 μM 5 d inhibits cell growth in a dose dependent manner 22090271
OCUT1 Function Assay 3 μm 24 h causes a dramatic increase in G2/M phase 22090271
CaOV3 Cell Viability Assay 1/5/10 μM 48 h decreases cell viability in a dose dependent manner cotreated with paclitaxel 21775054
SKOV3 Cytotoxicity Assay 5 μM 48 h enhances paclitaxel induced ovarian cancer cell death  21775054
A2780 Cytotoxicity Assay 5 μM 48 h enhances paclitaxel induced ovarian cancer cell death  21775054
HT-29  Cytotoxicity Assay 5 μM 48 h enhances paclitaxel induced ovarian cancer cell death  21775054
A498 Growth Inhibition Assay 0-40 μM 72 h inhibits cell growth in a dose dependent manner 21644050
CAKI-1 Growth Inhibition Assay 0-40 μM 72 h IC50~10 μM 21644050
769-P Growth Inhibition Assay 0-40 μM 72 h IC50~5-10 μM 21644050
786-0 Growth Inhibition Assay 0-40 μM 72 h IC50~5 μM 21644050
786-O Growth Inhibition Assay 0-20 μM 72 h inhibits cell growth in a dose dependent manner 21644050
CAKI-1 Growth Inhibition Assay 0-20 μM 72 h inhibits cell growth in a dose dependent manner 21644050
769-P Growth Inhibition Assay 0-20 μM 72 h inhibits cell growth in a dose dependent manner 21644050
A498 Growth Inhibition Assay 0-20 μM 72 h inhibits cell growth in a dose dependent manner 21644050
CWR22RV1 Cell Viability Assay 10 μM 24 h increases sensitivity of human CWR22RV1 cells to radiation 21496273
CWR22RV1 Apoptosis Asssay 10 μM 24 h enhances radiation induced apoptosis 21496273
CWR22RV1 Function Assay 5 μM 24 h reduced phosphorylation of Akt significantly 21496273
HepG2  Growth Inhibition Assay 5/10/20/40 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 20842425
Bel-7402 Growth Inhibition Assay 5/10/20/40 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 20842425
HepG2  Function Assay 5/10/20 μM 24 h results in the accumulation of cell number in the G2/M phase 20842425
Bel-7402 Function Assay 5/10/20 μM 24 h results in the accumulation of cell number in the G2/M phase 20842425
HepG2  Apoptosis Asssay 5/10/20 μM 24/48 h induces apoptosis at the long-time exposure 20842425
Bel-7402 Apoptosis Asssay 5/10/20 μM 24/48 h induces apoptosis at the long-time exposure 20842425
OAW-42 Growth Inhibition Assay 0-40 μM 72 h IC50~10 μM, inhibits cell growth in a dose dependent manner 20405296
PA-1  Growth Inhibition Assay 0-40 μM 72 h IC50~25 μM, inhibits cell growth in a dose dependent manner 20405296
SKOV3  Growth Inhibition Assay 0-40 μM 72 h IC50~30 μM, inhibits cell growth in a dose dependent manner 20405296
A2780 Growth Inhibition Assay 0-20 μM 48/72 h IC50 = 3 μm 20405296
A2780cis  Growth Inhibition Assay 0-20 μM 48/72 h IC50 = 6 μm 20405296
SKW6.4 Growth Inhibition Assay 2-10 μM 48 h inhibits cell growth in a dose dependent manner 20130960
MAVER Growth Inhibition Assay 2-10 μM 48 h inhibits cell growth in a dose dependent manner 20130960
BJAB Growth Inhibition Assay 2-10 μM 48 h inhibits cell growth in a dose dependent manner 20130960
OCI Growth Inhibition Assay 2-10 μM 48 h inhibits cell growth in a dose dependent manner 20130960
MOLM Growth Inhibition Assay 2-10 μM 48 h inhibits cell growth in a dose dependent manner 20130960
HL-60 Growth Inhibition Assay 2-10 μM 48 h inhibits cell growth in a dose dependent manner 20130960
SKW6.4 Apoptosis Asssay 10 μM 24/48 h induces apoptosis time-dependently 20130960
MAVER Apoptosis Asssay 10 μM 24/48 h induces apoptosis time-dependently 20130960
BJAB Apoptosis Asssay 10 μM 24/48 h induces apoptosis time-dependently 20130960
OCI Apoptosis Asssay 10 μM 24/48 h induces apoptosis time-dependently 20130960
MOLM Apoptosis Asssay 10 μM 24/48 h induces apoptosis time-dependently 20130960
HL-60 Apoptosis Asssay 10 μM 24/48 h induces apoptosis time-dependently 20130960
MGC803  Function Assay 0.75/10 μM 48 h decreases p-Akt (Ser 473), p-GSK3β (Ser 9), and C-MYC levels  23912246
SGC7901  Function Assay 0.75/10 μM 48 h decreases p-Akt (Ser 473), p-GSK3β (Ser 9), and C-MYC levels  23912246
U87MG Cell Viability Assay 0-25 μM 24-96 h decreases cell viability in both dose and time dependent manner 24065522
AsPC-1 Function Assay 0.5 μM 24 h inhibits Akt, S6K1, and Erk1/2 phosphorylation  24519751
MIA Function Assay 0.5 μM 24 h inhibits Akt, S6K1, and Erk1/2 phosphorylation  24519751
PANC-1 Function Assay 0.5 μM 24 h inhibits Akt, S6K1, and Erk1/2 phosphorylation  24519751
AsPC-1 Growth Inhibition Assay 0-25 μM 72 h inhibits cell growth in a dose dependent manner 24519751
MIA Growth Inhibition Assay 0-25 μM 72 h inhibits cell growth in a dose dependent manner 24519751
PANC-1 Growth Inhibition Assay 0-25 μM 72 h inhibits cell growth in a dose dependent manner 24519751
Ema Growth Inhibition Assay 0.1–100 μM 48 h IC50=58.7 μM 24881508
UL-1 Growth Inhibition Assay 0.1–100 μM 48 h IC50=7.01 μM 24881508
CLBL-1 Growth Inhibition Assay 0.1–100 μM 48 h IC50=33.0 μM 24881508
GL-1 Growth Inhibition Assay 0.1–100 μM 48 h IC50=9.91 μM 24881508
MDA-MB-231  Growth Inhibition Assay 0-10 μM 48 h EC50=1.13 ± 0.07 μM 25293576
HCC1806 Growth Inhibition Assay 0-10 μM 48 h EC50=2.84 ± 0.07 μM 25293576
RMG2 Apoptosis Asssay 30 μM 24 h induces apoptosis 25519148
RMG1 Apoptosis Asssay 30 μM 24 h induces apoptosis 25519148
A2780 Cell Viability Assay 1-30 μM 48 h decreases cell viability in a dose dependent manner 25519148
SKOV3 Cell Viability Assay 1-30 μM 48 h decreases cell viability in a dose dependent manner 25519148
OVISE Cell Viability Assay 1-30 μM 48 h decreases cell viability in a dose dependent manner 25519148
RMG2 Cell Viability Assay 1-30 μM 48 h decreases cell viability in a dose dependent manner 25519148
HAC2 Cell Viability Assay 1-30 μM 72 h decreases cell viability in a dose dependent manner 25519148
KOC7C Cell Viability Assay 1-30 μM 72 h decreases cell viability in a dose dependent manner 25519148
RMG2 Cell Viability Assay 1-30 μM 72 h decreases cell viability in a dose dependent manner 25519148
RMG1 Cell Viability Assay 1-30 μM 72 h decreases cell viability in a dose dependent manner 25519148
H460 Function Assay 3 μM 8 h blocks mTORC1, and ERK-MAPK activation combined with MEK-162 25697899
A549 Function Assay 3 μM 8 h blocks mTORC1, and ERK-MAPK activation combined with MEK-162 25697899
H460 Function Assay 3 μM 8 h blocks AKT activation 25697899
A549 Function Assay 3 μM 8 h blocks AKT activation 25697899
H460 Apoptosis Asssay 1/3 μM 48 h induces apoptosis 25697899
A549 Apoptosis Asssay 1/3 μM 48 h induces apoptosis 25697899
H460 Growth Inhibition Assay 0.3-10 μM 24/72 h inhibits cell growth in both time and dose dependent manner 25697899
A549 Growth Inhibition Assay 0.3-10 μM 24/72 h inhibits cell growth in both time and dose dependent manner 25697899
U-87 MG  Growth Inhibition Assay 20/40 μM 24/48 h inhibits cell growth in both time and dose dependent manner 25934232
HepG2 Growth Inhibition Assay 20/40 μM 24/48 h inhibits cell growth in both time and dose dependent manner 25934232
U-87 MG  Function Assay 20 μM 6/24 h increases the autophagic flux at 6 h while inhibits this flux at 24h 25934232
HepG2 Function Assay 20 μM 6/24 h decreases LC3-II degradation from 6 h 25934232
U-87 MG  Function Assay 20 μM 6/24 h increases the levels of LC3-II cotreated with CQ 25934232
HepG2 Function Assay 20 μM 6/24 h increases the levels of LC3-II cotreated with CQ 25934232
U-87 MG  Function Assay 20 μM 24 h increases double-membrane bound structures 25934232
HepG2 Function Assay 20 μM 24 h produces an intense cytoplasmic vacuolization corresponding to a notable dilatation of the ER cisterns 25934232
T24 BC  Apoptosis Asssay 2.5 μM 24 h sensitizes BC cells to sorafenib-induced apoptotic  26097873
T24 BC  Cell Viability Assay 0.5/1/2.5 μM 24 h enhances sorafenib-induced cell viability decrease 26097873
T24 BC  Function Assay 0.5/1/2.5 μM 3 h reduces the basal CB tyrosine phosphorylation levels in a dose-dependent manner 26097873
A549 Function assay 30 mins Inhibition of Akt phosphorylation in insulin-stimulated human A549 cells treated 2 hrs before insulin stimulation measured after 30 mins by ELISA, IC50=5.3μM 22138309
A549 Cytotoxicity assay 24 hrs Cytotoxicity against human A549 cells after 24 hrs by FACS analysis, IC50=7μM 22138309
KATO III Cytotoxicity assay 24 hrs Cytotoxicity against human KATO III cells after 24 hrs by FACS analysis, IC50=12.8μM 22138309
MCF7 Cytotoxicity assay 24 hrs Cytotoxicity against human MCF7 cells after 24 hrs by FACS analysis, IC50=13.3μM 22138309
A549 Function assay 2 hrs Inhibition of Akt phosphorylation in human insulin-stimulated A549 cells incubated for 2 hrs prior to insulin-induction measured after 30 mins by ELISA, IC50=5.3μM 23415083
PC3 Growth inhibition assay 48 hrs Growth inhibition of human PC3 cells after 48 hrs by SRB assay, GI50=0.44μM 24095759
NUGC3 Growth inhibition assay 48 hrs Growth inhibition of human NUGC3 cells after 48 hrs by SRB assay, GI50=0.54μM 24095759
HCT15 Growth inhibition assay 48 hrs Growth inhibition of human HCT15 cells after 48 hrs by SRB assay, GI50=1.25μM 24095759
MDA-MB-231 Growth inhibition assay 48 hrs Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay, GI50=2.86μM 24095759
NCI-H23 Growth inhibition assay 48 hrs Growth inhibition of human NCI-H23 cells after 48 hrs by SRB assay, GI50=4.21μM 24095759
ACHN Growth inhibition assay 48 hrs Growth inhibition of human ACHN cells after 48 hrs by SRB assay, GI50=4.56μM 24095759
A549 Cytotoxicity assay 24 to 72 hrs Cytotoxicity against human A549 cells after 24 to 72 hrs by haemocytometry, IC50=4.17μM 24900620
OVCAR8 Growth Inhibition Assay IC50=31.1 μM 23877012
HeyA8 Growth Inhibition Assay IC50=24.3 μM 23877012
A2780CP Growth Inhibition Assay IC50=7.6 μM 23877012
OVCAR5 Growth Inhibition Assay IC50=6.7 μM 23877012
A2780S Growth Inhibition Assay IC50=14.5 μM 23877012
MCAS Growth Inhibition Assay IC50=12.5 μM 23877012
M41R Growth Inhibition Assay IC50=19.8 μM 23877012
M41 Growth Inhibition Assay IC50=24.7 μM 23877012
TykNuR Growth Inhibition Assay IC50=5.5 μM 23877012
TykNu Growth Inhibition Assay IC50=3.5 μM 23877012
RBL2H3 Function assay Toxicity in rat RBL2H3 cells, MTD=25μM 20153565
PC3 Growth inhibition assay Growth inhibition of human PC3 cells by sulforhodamine B assay, GI50=0.44μM 21543141
NUGC3 Growth inhibition assay Growth inhibition of human NUGC3 cells by sulforhodamine B assay, GI50=0.54μM 21543141
HCT15 Growth inhibition assay Growth inhibition of human HCT15 cells by sulforhodamine B assay, GI50=1.25μM 21543141
MDA-MB-231 Growth inhibition assay Growth inhibition of human MDA-MB-231 cells by sulforhodamine B assay, GI50=2.86μM 21543141
NCI-H23 Growth inhibition assay Growth inhibition of human NCI-H23 cells by sulforhodamine B assay, GI50=4.21μM 21543141
ACHN Growth inhibition assay Growth inhibition of human ACHN cells by sulforhodamine B assay, GI50=4.56μM 21543141
PC3 Growth inhibition assay Growth inhibition of human PC3 cells by SRB assay, GI50=0.44μM 23266181
NUGC3 Growth inhibition assay Growth inhibition of human NUGC3 cells by SRB assay, GI50=0.54μM 23266181
HCT15 Growth inhibition assay Growth inhibition of human HCT15 cells by SRB assay, GI50=1.25μM 23266181
MDA-MB-231 Growth inhibition assay Growth inhibition of human MDA-MB-231 cells by SRB assay, GI50=2.86μM 23266181
NCI-H23 Growth inhibition assay Growth inhibition of human NCI-H23 cells by SRB assay, GI50=4.21μM 23266181
ACHN Growth inhibition assay Growth inhibition of human ACHN cells by SRB assay, GI50=4.56μM 23266181
A549 Cytotoxicity assay Cytotoxicity against human A549 cells by flow cytometric analysis, IC50=7μM 23415083
KATO III Cytotoxicity assay Cytotoxicity against human KATO III cells by flow cytometric analysis, IC50=12.8μM 23415083
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells by flow cytometric analysis, IC50=13.3μM 23415083
PC3 Antiproliferative assay Antiproliferative activity against human PC3 cells by SRB assay, GI50=0.44μM 23567950
NUGC3 Antiproliferative assay Antiproliferative activity against human NUGC3 cells by SRB assay, GI50=0.54μM 23567950
HCT15 Antiproliferative assay Antiproliferative activity against human HCT15 cells by SRB assay, GI50=1.25μM 23567950
MDA-MB-231 Antiproliferative assay Antiproliferative activity against human MDA-MB-231 cells by SRB assay, GI50=2.86μM 23567950
NCI-H23 Antiproliferative assay Antiproliferative activity against human NCI-H23 cells by SRB assay, GI50=4.21μM 23567950
ACHN Antiproliferative assay Antiproliferative activity against human ACHN cells by SRB assay, GI50=4.56μM 23567950
Rosetta cells Function assay Inhibition of wild-type human P38alpha MAPK expressed in Escherichia coli Rosetta cells, IC50=1.2μM 31274316
点击查看更多细胞系数据

生物活性

产品描述 Perifosine是一种新型的Akt抑制剂,在MM.1S细胞中IC50为4.7 μM,靶向作用于Akt的pleckstrin同源结构域。Phase 3。
靶点
Akt [1]
(MM.1S cells)
4.7 μM
体外研究(In Vitro)
体外研究活性

Perifosine抑制永生化角质形成细胞(HaCaT细胞)和头颈部鳞状癌细胞增值,IC50 为0.6-8.9 μM。[1] Perifosine极力减少Akt的磷酸化水平和细胞外信号调节激酶(ERK)1/2,诱导细胞周期停滞在G1和G2,并引起的小鼠的神经胶质祖细胞的剂量依赖性生长抑制。[2] Perifosine (10 μM) 完全抑制MM.1S细胞中Akt的磷酸化。[3] 最近的一项研究表明Perifosine通过阻断Akt的磷酸化诱导人类肝癌细胞中细胞周期停滞和细胞凋亡。[4]

激酶实验 Akt激酶活性
在MM.1S细胞中添加或不添加Perifosine(5 μM,6小时),然后用IL-6(20 ng/mL,10分钟)刺激。体外Akt激酶活性测定试验使用Akt激酶检测试剂盒。
细胞实验 细胞系 人脑胶质瘤细胞系
浓度 0, 15, 30和45 μM
孵育时间 48小时
方法

细胞在含10%FCS的培养基中培养48小时,添加不同浓度的Periosine。细胞活力通过3-(4,5 - 二甲基吡啶-2-基)-2,5-二苯基溴化镁(MTT)法确定。 (细胞增殖试剂盒I;罗氏)。在590nm处的吸光度是用96孔读板仪记录。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-AKT / AKT / p-S6K1 / S6K1 PARP p-mTOR / mTOR / Raptor / Rictor / p-p70S6K / p70S6K / p-4EBP1 / 4EBP1 / c-Myc / Cyclin D1 p-PDK1 / p-GSK3α/β / p-S6R 25519148
Growth inhibition assay Cell viability 28332584
体内研究(In Vivo)
体内研究活性

Perifosine联用在体内可减少肿瘤的增殖(PDGF驱动胶质瘤发生)。结果表明,Perifosine是一种有效抑制神经胶质瘤的药物并且可能是治疗神经胶质瘤的候选药物,在神经胶质瘤中的Akt和Ras-ERK1/2途径常常被激活。[2] 与PBS处理的对照动物相比,日服和周服Perifosine显著减少人MM肿瘤的生长并提高成活率。[3] Perifosine诱导血小板和白细胞增多,增加髓小鼠骨髓和脾脏,而它会导致移植骨髓瘤的凋亡。[5]

动物实验 Animal Models MM.1S MM细胞在BNX裸鼠(5〜6周龄)的右腰部皮下接种。
Dosages 250 mg/kg/wk或者36 mg/kg/d
Administration 口服
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01224730 Completed
Cancer
AEterna Zentaris
January 24 2012 Phase 1
NCT01049841 Completed
Pediatric Solid Tumors
Memorial Sloan Kettering Cancer Center|University of Wisconsin Madison|Duke University|NATL COMP CA NETWORK|Pfizer|AEterna Zentaris
January 2010 Phase 1
NCT01048580 Completed
Colon Cancer
AEterna Zentaris|SCRI Development Innovations LLC
October 2009 Phase 1
NCT00776867 Completed
Solid Tumors
Memorial Sloan Kettering Cancer Center|University of Wisconsin Madison|Duke University|AEterna Zentaris
October 2008 Phase 1

化学信息&溶解度

分子量 461.66 分子式

C25H52NO4P

CAS号 157716-52-4 SDF Download Perifosine SDF
Smiles CCCCCCCCCCCCCCCCCCOP(=O)([O-])OC1CC[N+](CC1)(C)C
储存条件(自收到货起)

体外溶解度
批次:

Water : 92 mg/mL (199.28 mM)

Ethanol : 92 mg/mL (199.28 mM)

DMSO : Insoluble ( ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

* 必填项

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们
Tags: buy Perifosine | Perifosine supplier | purchase Perifosine | Perifosine cost | Perifosine manufacturer | order Perifosine | Perifosine distributor
在线咨询
联系我们