Perifosine (KRX-0401)

Catalog No.S1037 Synonyms: NSC639966

Perifosine (KRX-0401) Chemical Structure

Molecular Weight(MW): 461.66

Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.

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Cited by 49 Publications

16 Customer Reviews

  • Tumor growth of 827 GSC-derived xenografts treated with an AKT inhibitor perifosine (30 mg/kg body weight). Twenty-three days after tumor implantation in mice, perifosine was administered by intraperitoneal injection (daily for 5 days). Error bars represent SD. Five mice per group, *p < 0.01.

    Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck.

    Immunoblot analysis of pY-STAT3, EZH2, AKT, and trimethylated H3K27 in lysates from xenograft tumors treated with an AKT inhibitor perifosine.

    Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck.

  • Co-IP analysis of methylated STAT3 in GBM xenograft tumors treated with perifosine.AKT inhibition in vivo decreased STAT3 methylation and pY-STAT3, but increased global levels of H3K27 trimethylation.

    Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck.

    IF staining of pS21 EZH2 and pY-STAT3 on the frozen sections of GBM xenografts treated with vehicle or perifosine. Nuclei were stained with DAPI. Bar represents 10 microns.

    Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck.

  • NRP-152 cells were transfected with Id1-luciferase reporter element as described in the figure and then incubated with±perifosine (10 nmol/L)  for 2 hours, followed by±LR3-IGF-I (10 nmol/L) for 24 hours. Cells were then treated with ±BMP4 and assayed for luciferase 2 hours later.

     

     

    Cancer Res 2010 70, 9106-9117. Perifosine (KRX-0401) purchased from Selleck.

     

    LAT2 is degraded by proteasomes after treatment with alkylphospholipids. A, 3-h treatment of NB4 cells before exposure to the proteasome inhibitor MG132 (10 μM) prevented the reduction of LAT2 induced by 25 μM ODPC. B, C, a similar effect was observed after exposure (30 min) of NB4 cells to the proteasome inhibitor MLN9708 (5 μM) followed by treatment with 25 μM ODPC (B) or 25 μM perifosine (C).

    Mol Cell Proteomics 2012 11(12), 1898-1912 . Perifosine (KRX-0401) purchased from Selleck.

  • (a) Validation of the global proteome and acetylome results. AS and BE2 cells were treated with 10 μM of perifosine for 16 h. Total proteins were extracted and 30 μg of protein was analyzed for integrin β5 and acetyl-Histone H2B (Lys12) by western blotting. GAPDH was used as loading control.

    Sci Rep, 2017, 7:41950. Perifosine (KRX-0401) purchased from Selleck.

    Alkylphospholipid-induced morphological changes in HepG2 cells. Cell morphology was examined with an inverted microscope(20× original magnification). The morphology of HepG2 cells incubated with MEM/10% FBS is shown in the absence of any addition (control, A), or in the presence of 25 μM of HePC (B), edelfosine (C), ErPC (D) or perifosine (E) for 24 h. ErPC, erucylphosphocholine; FBS, fetal bovine serum; HePC, hexadecylphosphocholine; MEM, minimal essential medium.

     

     

    Brit J Pharmacol 2010 160, 355–366. Perifosine (KRX-0401) purchased from Selleck.

  • Knockdown of BRCA1 sensitizes cells to PI3K/AKT pathway inhibitors. MCF7 cells transfected with either BRCA1-siRNA or control-siRNA were treated with increasing amounts of inhibitors targeting the PI3K/AKT pathway for 48 h in triplicate. Viable cells were measured by MTT assay.

    Mol Carcinog 2012 ahead of print. Perifosine (KRX-0401) purchased from Selleck.

    Established cell lines (A549 and H460 lines) were un-stimulated (“C”, same for all figures), or treated with indicated concentration of perifosine (0.3-10 μM) or plus ABT-737 (100 nM), cells were then cultured for indicated time, and cell growth was tested by MTT assay (a, b, d, e) or by colony formation assay (c and f). “Prf” stands for perifosine (Same for all figures). The results presented were representative of three independent experiments. The values were expressed as the means ± SD. *p < 0.05 vs “C” group. #p < 0.05 compared with the perifosine only group without ABT-737 co-treatment.

    Biochem Biophys Res Commun, 2016, 473(4):1170-6. Perifosine (KRX-0401) purchased from Selleck.

  • Western blotting analysis demonstrating Ser473p-Akt and total Akt levels in HepG2 cells and Bel-7402 cells treated with increasing concentrations of perifosine for 24 h. Betaactin served as loading control. Bands were analyzed by Glyco Band-Scan software. Each bar corresponds to the mean ±SD for at least three independent experiments. * P<0.05,** P<0.01 vs. control, Student,s t test

     

     

    Cytotechnology 2010 62, 449-460. Perifosine (KRX-0401) purchased from Selleck.

    Induction of apoptosis in hepatoma cells by treatment for 48 h with 10 μM perifosine. The treated cells were stained with DAPI and the apoptotic morphological changes in the nuclear chromatin were observed under a fluorescent microscope.

    Cytotechnology 2010 62, 449-460. Perifosine (KRX-0401) purchased from Selleck.

  • Western blotting assay showing cleavage of caspase-3, caspase-9 and PARP in response to perifosine treatment in hepatoma cells. Each bar corresponds to the mean ±SD for at least three independent experiments. * P<0.05, ** P<0.01 vs. control, Student,s t test

    Cytotechnology 2010 62, 449-460. Perifosine (KRX-0401) purchased from Selleck.

    This chart showed the change of the stable transfection cells in centrosome separation after the cells were treated with perifosine(1 μM)  6 hours, 12 hours and 24 hours. "C" means the control group, and "P" means the group treated with perifosine

    2010 Zhao Jing PHD Medical College of Peking University. Perifosine (KRX-0401) purchased from Selleck.

  • TEIF (telomerase transcriptional elements-interacting factor)gene is a novel human gene and cloned from the expression library of  HeLa cell through the hTERT promoter-based yeast one-hybrid assay. And now we are trying to find the interaction between TEIF and the EGF pathway.

     

     

    2010 Zhao Jing PHD Medical College of Peking University . Perifosine (KRX-0401) purchased from Selleck.

     After starved in serum-free medium for 24h,T47D cells incubated with the indicated concentrations of Perifosine for 3h,followed by 15-minute  stimolation of 100ng/ml EGF.

     

     

     

    2010 Dr. Zhang of Tianjin Medical University. Perifosine (KRX-0401) purchased from Selleck.

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Biological Activity

Description Perifosine (KRX-0401) 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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T24 BC  M3XhcmZ2dmO2aX;uJGF{e2G7 MkH0NE42NzFxMj61JO69VQ>? NYLiZWZ3OyCq NUTZW3ZpemWmdXPld{B1cGViYnHzZYwhS0JidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKGyndnXsd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGfNSY0zPjB7N{i3Ny=>
T24 BC  NWDIb2hzS2WubDDWbYFjcWyrdImgRZN{[Xl? NYTrcHptOC53L{GvNk42KM7:TR?= MkW1NlQhcA>? MVvlcohidmOnczDzc5Ji\mWwaXKtbY5lfWOnZDDj[YxtKH[rYXLpcIl1gSCmZXPy[YF{\Q>? NXrVWHdEOjZyOUe4O|M>
T24 BC  NYXN[4w6SXCxcITvd4l{KEG|c4PhfS=> M2[0UVIvPSEQvF2= M3P3TVI1KGh? M3\Td5NmdnOrdHn6[ZMhSkNiY3XscJMhfG9ic3;yZYZmdmmkLXnu[JVk\WRiYYDvdJRwfGmlwrC= MWCyOlA6Pzh5Mx?=
HepG2 M1rYdmZ2dmO2aX;uJGF{e2G7 NWnnV|BwOjEEoN88US=> MmHzNlTDqGh? MVTwdo9lfWOnczDhckBqdnSnboPlJIN6fG:ybHHzcYlkKH[jY4XvcIl7[XSrb36gZ49zemW|cH;u[Ilv\yC2bzDhJI5wfGGkbHWg[Ilt[XSjdHnvckBw\iC2aHWgSXIh[2m|dHXycpM> MV[yOVk{PDJ|Mh?=
U-87 MG  NUX1UYl3TnWwY4Tpc44hSXO|YYm= NHfkfWUzOMLizszN MXyyOOKhcA>? NIDs[JNqdmO{ZXHz[ZMh\G:3YnzlMY1mdWK{YX7lJIJwfW6mIIP0dpVkfHW{ZYO= MkS4NlU6OzR{M{K=
HepG2 MV;GeY5kfGmxbjDBd5NigQ>? NIHa[4EzOMLizszN NGjFNnM3NzJ2IHi= NEXWc|NqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjDMR|MuUUliY3;0doVifGWmIIfpeIghS1F? NXH6R3JKOjV7M{SyN|I>
U-87 MG  M4Lk[2Z2dmO2aX;uJGF{e2G7 NVflUXM1OjEEoN88US=> NIDtR4Q3NzJ2IHi= NWLmdINMcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[gUGM{NUmLIHPveJJm[XSnZDD3bZRpKEOT NU[yd4lqOjV7M{SyN|I>
HepG2 M3S1V2Z2dmO2aX;uJGF{e2G7 MoXnNlDDqM7:TR?= MWG2M|I1KGh? MmTt[IVkemWjc3XzJGxEOy2LSTDk[Ydz[WSjdHnvcuKh\nKxbTC2JIg> M4jWXFI2QTN2MkOy
U-87 MG  M{i3S2Z2dmO2aX;uJGF{e2G7 NEDSTlEzOMLizszN M{jOd|YwOjRiaB?= NWjkPINjcW6lcnXhd4V{KHSqZTDheZRweGijZ3njJIZtfXhiIHH0JFYhcCC5aHns[UBqdmirYnn0d{B1cGm|IH\seZgh[XRiMkTo MXuyOVk{PDJ|Mh?=
HepG2 MojhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVyyNE81OCEQvF2= M2rz[VI1NzR6IHi= Mlv5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NXztfXV1OjV7M{SyN|I>
U-87 MG  NFLqRWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6yNE81OCEQvF2= NET2TFYzPC92ODDo NXrkUJo6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NVz0c2FUOjV7M{SyN|I>
A549 NWCyNYdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFv3Z4wxNjNvMUCg{txO MX2yOE84OiCq MnLibY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? Mk\tNlU3QTd6OUm=
H460 NX7zOmVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3XTmQxNjNvMUCg{txO NXHYdlRXOjRxN{KgbC=> NFnpe|RqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NEW2TFQzPTZ7N{i5PS=>
A549 M3LBcGFxd3C2b4Ppd{BCe3O|YYm= M33WSlEwOyEQvF2= NH\tN|g1QCCq NUPHVGxScW6mdXPld{BieG:ydH;zbZM> NVzCb|g4OjV4OUe4PVk>
H460 M1HkZ2Fxd3C2b4Ppd{BCe3O|YYm= NEjjXVYyNzNizszN MoXxOFghcA>? NH3NOIJqdmS3Y3XzJIFxd3C2b4Ppdy=> M{jBUlI2Pjl5OEm5
A549 MVPGeY5kfGmxbjDBd5NigQ>? MWmzJO69VQ>? NGewclA5KGh? NWfnUnR[[myxY3vzJGFMXCCjY4TpeoF1cW:w NYjCNFdrOjV4OUe4PVk>
H460 M{jWfmZ2dmO2aX;uJGF{e2G7 MWqzJO69VQ>? NYX5V4x{QCCq NVW4SJRH[myxY3vzJGFMXCCjY4TpeoF1cW:w NF;zbFAzPTZ7N{i5PS=>
A549 M{PDS2Z2dmO2aX;uJGF{e2G7 NYm1c3ZwOyEQvF2= M1rVR|ghcA>? MVvicI9kc3NibWTPVmMyNCCjbnSgSXJMNU2DUFugZYN1cX[jdHnvckBkd22kaX7l[EB4cXSqIF3FT{0yPjJ? NH;JRmczPTZ7N{i5PS=>
H460 MYfGeY5kfGmxbjDBd5NigQ>? NGrEe3M{KM7:TR?= MYe4JIg> MlfXZoxw[2u|IH3UU3JEOSxiYX7kJGVTUy2PQWDLJIFkfGm4YYTpc44h[2:vYnnu[YQhf2m2aDDNSWsuOTZ{ MmH4NlU3QTd6OUm=
RMG1 M1v5W2NmdGxiVnnhZoltcXS7IFHzd4F6 NHTXWVkyNTNyIN88US=> NXHCR4l2PzJiaB?= M1LnbIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MWqyOVUyQTF2OB?=
RMG2 M2[1[WNmdGxiVnnhZoltcXS7IFHzd4F6 NUm3TmFIOS1|MDFOwG0> M{XpUVczKGh? M{HjfoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M4HoUFI2PTF7MUS4
KOC7C M{\CdWNmdGxiVnnhZoltcXS7IFHzd4F6 NUTNc3BzOS1|MDFOwG0> MV63NkBp NWSxd3db\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MXGyOVUyQTF2OB?=
HAC2 NXLnU4hjS2WubDDWbYFjcWyrdImgRZN{[Xl? NEm2dmYyNTNyIN88US=> NHOyelE4OiCq M{i5WYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NVrFW5dqOjV3MUmxOFg>
RMG2 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUexMVMxKM7:TR?= M2HYZ|Q5KGh? M{HrOYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NEPvO3QzPTVzOUG0PC=>
OVISE MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYflUG1UOS1|MDFOwG0> M3ruWlQ5KGh? MnrX[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MkjoNlU2OTlzNEi=
SKOV3 MWLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEjwd2wyNTNyIN88US=> M4nMblQ5KGh? MWfk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M1vRdFI2PTF7MUS4
A2780 MoSyR4VtdCCYaXHibYxqfHliQYPzZZk> NVz5XZp[OS1|MDFOwG0> NHfUbHk1QCCq MUXk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NVjPbW9nOjV3MUmxOFg>
RMG1 MnXQRZBweHSxc3nzJGF{e3OjeR?= MmXCN|Ah|ryP MoDuNlQhcA>? MmDXbY5lfWOnczDhdI9xfG:|aYO= Mn;4NlU2OTlzNEi=
RMG2 MXvBdI9xfG:|aYOgRZN{e2G7 MnjqN|Ah|ryP M2fqN|I1KGh? NWPOdopkcW6mdXPld{BieG:ydH;zbZM> MUWyOVUyQTF2OB?=
HCC1806 M2nqSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:4RlAuOTBizszN MYW0PEBp MmO3SWM2OD1{Lki05qCKyrIkgJmwMlA4KM7:TR?= NH3CdpczPTJ7M{W3Oi=>
MDA-MB-231  MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\INE0yOCEQvF2= MoPhOFghcA>? NVzYeHNETUN3ME2xMlE{6oDLwsJihKkxNjB5IN88US=> M2fae|I2Ojl|NUe2
GL-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX6wMlHjiJNzMEFihKnPxE1? MofEOFghcA>? NH6wO|JKSzVyPUmuPVEh|ryP M3XYSFI1QDhzNUC4
CLBL-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV6wMlHjiJNzMEFihKnPxE1? NIP3d3c1QCCq NHnFXohKSzVyPUOzMlAh|ryP M{PKOFI1QDhzNUC4
UL-1 NXu5dnVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPEUFgxNjIkgKOxNFDjiIoQvF2= M3excVQ5KGh? MoTxTWM2OD15LkCxJO69VQ>? NVfTdXk6OjR6OEG1NFg>
Ema NFPzdW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4T3SlAvOeLCk{GwNQKBkc7:TR?= NYXZ[HdFPDhiaB?= M1X5SWlEPTB;NUiuO{DPxE1? Mk\WNlQ5QDF3MEi=
PANC-1 M1TSWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq3e5QxNTJ3IN88US=> NH3keoo4OiCq NYixOIlMcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MkPPNlQ2OTl5NUG=
MIA MojLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkCzNE0zPSEQvF2= M3jFUFczKGh? NGrVb5dqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MmXQNlQ2OTl5NUG=
AsPC-1 M1rlUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS4NE0zPSEQvF2= NVLBWIhsPzJiaB?= M2Lx[IlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MmnoNlQ2OTl5NUG=
PANC-1 MX7GeY5kfGmxbjDBd5NigQ>? MVGwMlUh|ryP M2rtOlI1KGh? MmPBbY5pcWKrdIOgRYt1NCCVNluxMEBidmRiRYLrNU8zKHCqb4PwbI9zgWyjdHnvcuKh NVexNpZGOjR3MUm3OVE>
MIA MoH4SpVv[3Srb36gRZN{[Xl? MkC5NE42KM7:TR?= MlyxNlQhcA>? MYrpcohq[mm2czDBb5QtKFN4S{GsJIFv\CCHcnuxM|IheGixc4Doc5J6dGG2aX;uxsA> MYiyOFUyQTd3MR?=
AsPC-1 NULNWGE{TnWwY4Tpc44hSXO|YYm= MmntNE42KM7:TR?= NHm3UWkzPCCq NVW2fWtlcW6qaXLpeJMhSWu2LDDTOmsyNCCjbnSgSZJsOS9{IIDoc5NxcG:{eXzheIlwdsLi M3LWUFI1PTF7N{Wx
U87MG NXTEemZ5S2WubDDWbYFjcWyrdImgRZN{[Xl? NImx[5cxNTJ3IN88US=> MWWyOE06PiCq NWThc|VI\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGKxdHig[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnRibXHucoVz MXGyOFA3PTV{Mh?=
SGC7901  NYn5dXdXTnWwY4Tpc44hSXO|YYm= Mnn6NE44PS9zMNMg{txO NWPWV4ZWPDhiaB?= NHjMRmNl\WO{ZXHz[ZMheC2Da4SgLHNmeiB2N{OpMEBxNUeVS{ROtkApW2W{IEmpMEBidmRiQz3NXWMhdGW4ZXzzxsA> NVzmbHVOOjN7MUKyOFY>
MGC803  MoXOSpVv[3Srb36gRZN{[Xl? M4DtRlAvPzVxMUFCpO69VQ>? NFXkNnM1QMLiaB?= Mljk[IVkemWjc3XzJJAuSWu2IDjT[ZIhPDd|KTygdE1IW0t|zsKgLHNmeiB7KTygZY5lKENvTWnDJIxmfmWuc9Mg NXWxPJpNOjN7MUKyOFY>
TykNu NIfYXlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnVNYdKSzVyPUOuOUDPxE1? Mn\rNlM5PzdyMUK=
TykNuR NWHieplCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\oephKSzVyPUWuOUDPxE1? M2\UbVI{QDd5MEGy
M41 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rNT2lEPTB;MkSuO{DPxE1? MXWyN|g4PzBzMh?=
M41R M1TE[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzNTWM2OD1zOT64JO69VQ>? NV3GdW84OjN6N{ewNVI>
OVCAR8 M4nHSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTNzLkGg{txO NXS5OmxGOjN6N{ewNVI>
HeyA8 NULEc3FqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTJ2LkOg{txO M2\nbVI{QDd5MEGy
A2780CP NEnpWXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlm4TWM2OD15Lk[g{txO NX\KeGRTOjN6N{ewNVI>
OVCAR5 M{PvVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37xbWlEPTB;Nj63JO69VQ>? NVKyb3FpOjN6N{ewNVI>
A2780S M{\GOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTF2LkWg{txO MXSyN|g4PzBzMh?=
MCAS NXjweWVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3Cc4E3UUN3ME2xNk42KM7:TR?= NVPDVIhMOjN6N{ewNVI>
NCI-H727 NILXb5lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mnj1NE0yODBizszN NEjVOlYzPC95MjDo MY\k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZo91cCCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueEBu[W6wZYK= NEezVoEzOjR7OUSzOy=>
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HepG2  NYD0U3pVSXCxcITvd4l{KEG|c4PhfS=> M{T6SVUwOTBxMkCg{txO NFf1bpczPC92ODDo NVmw[2tjcW6mdXPld{BieG:ydH;zbZMh[XRidHjlJIxwdmdvdHnt[UBmgHCxc4Xy[S=> M2LtdFIxQDR{NEK1
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SKW6.4 NH\jcJFCeG:ydH;zbZMhSXO|c3H5 NXrDWIlmOTEEoN88US=> NH6x[YUzPC92ODDo NWLKOos2cW6mdXPld{BieG:ydH;zbZMhfGmvZT3k[ZBmdmSnboTsfS=> NU\0VZFROjBzM{C5OlA>
MAVER M2PpUmFxd3C2b4Ppd{BCe3O|YYm= NVLrPFgyOTEEoN88US=> MljWNlQwPDhiaB?= Mk\rbY5lfWOnczDhdI9xfG:|aYOgeIlu\S2mZYDlcoRmdnSueR?= M13DT|IxOTNyOU[w
BJAB NWiwV3l2SXCxcITvd4l{KEG|c4PhfS=> MX:xNOKh|ryP MX2yOE81QCCq NHXncGZqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nLXTldIVv\GWwdHz5 MnztNlAyOzB7NkC=
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HL-60 Mlu4RZBweHSxc3nzJGF{e3OjeR?= MorZNVDDqM7:TR?= MkPRNlQwPDhiaB?= NH3reVJqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nLXTldIVv\GWwdHz5 MorjNlAyOzB7NkC=

... Click to View More Cell Line Experimental Data

In vivo Perifosine combining with temozolomide 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]

Protocol

Kinase Assay:[3]
+ Expand

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:[2]
+ Expand
  • 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 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. (Cell Proliferation Kit I; Roche). The absorbance at 590 nm is recorded using the 96-well plate reader.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: MM.1S MM cells are inoculated subcutaneously in the right flank of Beige-nude-xid (BNX) mice (5 to 6 weeks old).
  • Formulation: 0.9% NaCl solution
  • Dosages: 250 mg/kg/wk or 36 mg/kg/d
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 15 mg/mL (32.49 mM)
Water 8 mg/mL (17.32 mM)
DMSO Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
water
For best results, use promptly after mixing.
8mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 461.66
Formula

C25H52NO4P

CAS No. 157716-52-4
Storage powder
in solvent
Synonyms NSC639966

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02238496 Active, not recruiting Brain Tumor, Recurrent|Glioblastoma|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Mixed Glioma Andrew Lassman|Pfizer|AEterna Zentaris|Columbia University July 2014 Phase 2
NCT01224730 Unknown status Cancer AEterna Zentaris January 2012 Phase 1
NCT01097018 Completed Colorectal Cancer AEterna Zentaris April 2010 Phase 3
NCT01049841 Active, not recruiting 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
NCT01051557 Active, not recruiting Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Adult Diffuse Astrocytoma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Adult Oligodendroglioma|Recurrent Adult Brain Neoplasm National Cancer Institute (NCI) January 2010 Phase 1|Phase 2
NCT01002248 Terminated Multiple Myeloma AEterna Zentaris|Dana-Farber Cancer Institute December 2009 Phase 3

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID