Perifosine

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

目录号：S1037 Purity: 97%

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

CAS: 157716-52-4

规格	价格	库存
5mg	1220.79	现货
25mg	3849.3	现货
50mg	7117.44	现货
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产品质控

批次：纯度： >97%

Perifosine相关产品

相关靶点	Akt1 Akt2 Akt3	点击展开
相关产品	MK-2206 2HCl SC79 Capivasertib (AZD5363) GSK690693 Ipatasertib (GDC-0068) Triciribine (API-2) CCT128930 Afuresertib (GSK2110183) A-674563 HCl AT7867 Oridonin Akti-1/2 PHT-427 TIC10 (ONC201) Miransertib (ARQ 092) HCl AT13148 Uprosertib (GSK2141795) Miransertib (ARQ-092) SC66 Deguelin ML-9 HCl	点击展开
相关化合物库	激酶抑制剂库 PI3K/Akt 抑制剂库凋亡分子化合物库细胞周期化合物库 NF-κB信号通路库	点击展开

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
激酶实验	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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
[1] Vyomesh Patel, et al. Cancer Res, 2002, 62(5), 1401-1409 [2] Momota H, et al. Cancer Res, 2005, 65(16), 7429-7435. [3] Hideshima T, et al. Blood, 2006, 107(10), 4053-4062. [4] Fei HR, et al. Cytotechnology, 2010, 62(5), 449-460 [5] Catley L, et al. Exp Hematol, 2007, 32(7), 1038-1046 + 展开

参考文献

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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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

Water : 92 mg/mL (199.28 mM)

Ethanol : 92 mg/mL (199.28 mM)