Home PI3K/Akt/mTOR Akt inhibitor Perifosine For research use only.

Perifosine

Synonyms: KRX-0401, NSC639966, D21266

Perifosine is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.

Perifosine Chemical Structure

Perifosine Chemical Structure

CAS No. 157716-52-4

Purity & Quality Control

Perifosine Related Products

Signaling Pathway

Akt Signaling Pathways

Akt Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL-60 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
OCI 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
MAVER Apoptosis Asssay 10 μM 24/48 h induces apoptosis time-dependently 20130960
SKW6.4 Apoptosis Asssay 10 μM 24/48 h induces apoptosis time-dependently 20130960
HL-60 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
OCI 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
MAVER Growth Inhibition Assay 2-10 μM 48 h inhibits cell growth in a dose dependent manner 20130960
SKW6.4 Growth Inhibition Assay 2-10 μM 48 h inhibits cell growth in a dose dependent manner 20130960
A2780cis  Growth Inhibition Assay 0-20 μM 48/72 h IC50 = 6 μm 20405296
A2780 Growth Inhibition Assay 0-20 μM 48/72 h IC50 = 3 μm 20405296
SKOV3  Growth Inhibition Assay 0-40 μM 72 h IC50~30 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
OAW-42 Growth Inhibition Assay 0-40 μM 72 h IC50~10 μM, inhibits cell growth in a dose dependent manner 20405296
Bel-7402 Apoptosis Asssay 5/10/20 μM 24/48 h induces apoptosis at the long-time exposure 20842425
HepG2  Apoptosis Asssay 5/10/20 μM 24/48 h induces apoptosis at the long-time exposure 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  Function Assay 5/10/20 μM 24 h results in the accumulation of cell number in the G2/M phase 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  Growth Inhibition Assay 5/10/20/40 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 20842425
CWR22RV1 Function Assay 5 μM 24 h reduced phosphorylation of Akt significantly 21496273
CWR22RV1 Apoptosis Asssay 10 μM 24 h enhances radiation induced apoptosis 21496273
CWR22RV1 Cell Viability Assay 10 μM 24 h increases sensitivity of human CWR22RV1 cells to radiation 21496273
A498 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
CAKI-1 Growth Inhibition Assay 0-20 μM 72 h inhibits cell growth in a dose dependent manner 21644050
786-O Growth Inhibition Assay 0-20 μM 72 h inhibits cell growth in a dose dependent manner 21644050
786-0 Growth Inhibition Assay 0-40 μM 72 h IC50~5 μM 21644050
769-P Growth Inhibition Assay 0-40 μM 72 h IC50~5-10 μM 21644050
CAKI-1 Growth Inhibition Assay 0-40 μM 72 h IC50~10 μM 21644050
A498 Growth Inhibition Assay 0-40 μM 72 h inhibits cell growth in a dose dependent manner 21644050
HT-29  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
SKOV3 Cytotoxicity Assay 5 μM 48 h enhances paclitaxel induced ovarian cancer cell death  21775054
CaOV3 Cell Viability Assay 1/5/10 μM 48 h decreases cell viability in a dose dependent manner cotreated with paclitaxel 21775054
OCUT1 Function Assay 3 μm 24 h causes a dramatic increase in G2/M phase 22090271
K1 Growth Inhibition Assay 0.1-3 μM 5 d inhibits cell growth in a dose dependent manner 22090271
OCUT1 Growth Inhibition Assay 0.1-3 μM 5 d inhibits cell growth in a dose dependent manner 22090271
K562 Function Assay 20 μM 48 h induces autophagy  22407228
HL-60 Function Assay 2.5/5/10 μM 24 h induces the phosphorylation of JNK1/2 in a dose dependent manner 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 decreases Akt and p-Akt levels dose-dependently 22407228
Kasumi-1 Function Assay 2.5/5/10 μM 24 h decreases Akt and p-Akt levels dose-dependently 22407228
HL-60 Apoptosis Asssay 10 μM 24 h induces apoptosis 22407228
Kasumi-1 Apoptosis Asssay 10 μM 24 h induces apoptosis 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 Cell Viability Assay 0-20 μM 24/48 h decreases cell viability in both dose and time dependent manner 22407228
BON1 Function Assay 7.5/10 μM 8 h decreases the expression of the anti-apoptotic proteins BCL2 and Bcl-XL 22499437
BON1 Apoptosis Asssay 0-10 μM 24 h induces apoptosis dose dependently 22499437
BON1 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
NCI-H727 Cell Viability Assay 0-100 μM 24/72 h decreases cell viability in both dose and time dependent manner 22499437
MCAS Growth Inhibition Assay IC50=12.5 μM 23877012
A2780S Growth Inhibition Assay IC50=14.5 μM 23877012
OVCAR5 Growth Inhibition Assay IC50=6.7 μM 23877012
A2780CP Growth Inhibition Assay IC50=7.6 μM 23877012
HeyA8 Growth Inhibition Assay IC50=24.3 μM 23877012
OVCAR8 Growth Inhibition Assay IC50=31.1 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
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
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
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
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 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
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
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
Rosetta cells Function assay Inhibition of wild-type human P38alpha MAPK expressed in Escherichia coli Rosetta cells, IC50=1.2μM 31274316
Click to View More Cell Line Experimental Data

Biological Activity

Description Perifosine is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.
Targets
Akt [1]
(MM.1S cells)
4.7 μM
In vitro
In vitro

Perifosine develops anti-proliferative properties with IC50 of 0.6-8.9 μM in immortalized keratinocytes (HaCaT), and head and neck squamous carcinoma cells. [1] Perifosine strongly reduces phosphorylation levels of Akt and extracellular signal-regulated kinase (Erk) 1/2, induces cell cycle arrest in G1 and G2, and causes dose-dependent growth inhibition of mouse glial progenitors. [2] Perifosine (10 μM) completely inhibits the phosphorylation of Akt in MM.1S cells. [3] A recent study demonstrates Perifosine induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation. [4]
Kinase Assay Akt kinase assay
MM.1S cells are cultured in the presence or absence of perifosine (5 μM, 6 hours) and then stimulated with IL-6 (20 ng/mL, 10 minutes). In vitro akt kinase assay is then carried out using the Akt Kinase Assay Kit.
Cell Research Cell lines Human glioma cell lines
Concentrations 0, 15, 30 and 45 μM
Incubation Time 48 hours
Method

Cells are incubated in the medium with 10% FCS for 48 hours with indicated concentration of Periosine. Cell viability is determined by the MTT assay. (Cell Proliferation Kit I; Roche). The absorbance at 590 nm is recorded using the 96-well plate reader.
Experimental Result Images Methods Biomarkers Images 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
In Vivo
In vivo

Perifosine in combination reduces tumor proliferation (a PDGF-driven gliomagenesis) in vivo. The results indicate that Perifosine is an effective drug in gliomas in which Akt and Ras-Erk 1/2 pathways are frequently activated, and may be new candidate for glima treatment in the clinic. [2] Both oral daily and weekly administration of Perifosine significantly reduce human MM tumor growth and increase survival, compared with control animals treated with PBS vehicle only. [3] Perifosine induces thrombocytosis and leukocytosis and increases myelopoiesis in murine marrow and spleen, whereas it causes apoptosis in myeloma xenografts. [5]
Animal Research Animal Models MM.1S MM cells are inoculated subcutaneously in the right flank of Beige-nude-xid (BNX) mice (5 to 6 weeks old).
Dosages 250 mg/kg/wk or 36 mg/kg/d
Administration Oral gavage
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

Chemical Information & Solubility

Molecular Weight 461.66 Formula

C25H52NO4P
CAS No. 157716-52-4 SDF Download Perifosine SDF
Smiles CCCCCCCCCCCCCCCCCCOP(=O)([O-])OC1CC[N+](CC1)(C)C
Storage (From the date of receipt)

In vitro
Batch:

Water : 92 mg/mL

Ethanol : 92 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Perifosine | Perifosine supplier | purchase Perifosine | Perifosine cost | Perifosine manufacturer | order Perifosine | Perifosine distributor