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  MXzGeY5kfGmxbjDBd5NigQ>? NGLIPWwxNjVxMT:yMlUh|ryP NEG3SYM{KGh? MmLndoVlfWOnczD0bIUh[mG|YXygR2IhfHm{b4PpcoUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MnmwNlYxQTd6N{O=
T24 BC  MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1;WV|AvPS9zL{KuOUDPxE1? MYOyOEBp Mnfo[Y5p[W6lZYOgd49z[W[nbnniMYlv\HWlZXSgZ4VtdCC4aXHibYxqfHliZHXjdoVie2V? Mlf5NlYxQTd6N{O=
T24 BC  NVm5[5dqSXCxcITvd4l{KEG|c4PhfS=> NFTJSngzNjVizszN MUKyOEBp NW\TTItoe2Wwc3n0bZpmeyCEQzDj[YxteyC2bzDzc5Ji\mWwaXKtbY5lfWOnZDDhdI9xfG:2aXRCpC=> MV[yOlA6Pzh5Mx?=
HepG2 MWPGeY5kfGmxbjDBd5NigQ>? NUHSenZOOjEEoN88US=> M1\ub|I1yqCq M1fwc5Bzd2S3Y3XzJIFvKGmwdHXud4Uh[3m2b4DsZZNucWNidnHjeY9tcXqjdHnvckBkd3K{ZYPwc45lcW6pIITvJIEhdm:2YXLs[UBlcWyjdHH0bY9vKG:oIITo[UBGWiClaYP0[ZJvew>? NYTJS4t3OjV7M{SyN|I>
U-87 MG  NEHaT|JHfW6ldHnvckBCe3OjeR?= MX2yNOKh|ryP MoqxNlTDqGh? Mm\ibY5kemWjc3XzJIRwfWKuZT3t[Y1jemGwZTDic5Vv\CC|dIL1Z5R2emW| NWf0OnZDOjV7M{SyN|I>
HepG2 MW\GeY5kfGmxbjDBd5NigQ>? Mn30NlDDqM7:TR?= M2rZeFYwOjRiaB?= MoTObY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZiTFOzMWlKKGOxdILlZZRm\CC5aYToJGNS M2H4[|I2QTN2MkOy
U-87 MG  M{D1V2Z2dmO2aX;uJGF{e2G7 NGPweHIzOMLizszN M1vUS|YwOjRiaB?= M3LsTYlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIFzDN{1KUSClb4Ty[YF1\WRid3n0bEBEWQ>? NV\TTJdMOjV7M{SyN|I>
HepG2 MUPGeY5kfGmxbjDBd5NigQ>? M1TBNVIxyqEQvF2= Mn3KOk8zPCCq M{jXS4Rm[3KnYYPld{BNSzNvSVmg[IVoemGmYYTpc47DqG[{b32gOkBp M37vfVI2QTN2MkOy
U-87 MG  NFrw[lZHfW6ldHnvckBCe3OjeR?= MofONlDDqM7:TR?= M4LsflYwOjRiaB?= NIP2SpJqdmO{ZXHz[ZMhfGinIHH1eI9xcGGpaXOg[ox2gCBiYYSgOkBpKHeqaXzlJIlvcGmkaYTzJJRpcXNiZnz1fEBifCB{NHi= MoO5NlU6OzR{M{K=
HepG2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfWSWg2OjBxNECg{txO MmDENlQwPDhiaB?= NEPYNVdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MYOyOVk{PDJ|Mh?=
U-87 MG  MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjETHFVOjBxNECg{txO MVeyOE81QCCq MYHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M2ewTVI2QTN2MkOy
A549 Mk\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWD6[XgxOC5|LUGwJO69VQ>? M17FNVI1Nzd{IHi= M3XOeYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NWLPXIJPOjV4OUe4PVk>
H460 NWPsdWJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfGbIIxNjNvMUCg{txO MlzDNlQwPzJiaB?= NW\Gb3UzcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NFLlS4wzPTZ7N{i5PS=>
A549 M1;2SmFxd3C2b4Ppd{BCe3O|YYm= M4\1dFEwOyEQvF2= MnvpOFghcA>? NYnxXmZxcW6mdXPld{BieG:ydH;zbZM> NXrBUXY2OjV4OUe4PVk>
H460 NGrwb4JCeG:ydH;zbZMhSXO|c3H5 NGHFd2MyNzNizszN M3vZOVQ5KGh? M17reYlv\HWlZYOgZZBweHSxc3nz M3ewNlI2Pjl5OEm5
A549 NXfCe2puTnWwY4Tpc44hSXO|YYm= MmTRN{DPxE1? NF21U5A5KGh? NWrLO|hs[myxY3vzJGFMXCCjY4TpeoF1cW:w NIniXlMzPTZ7N{i5PS=>
H460 NWfiW4tMTnWwY4Tpc44hSXO|YYm= MWezJO69VQ>? MXi4JIg> M4T3WYJtd2OtczDBT3Qh[WO2aY\heIlwdg>? MlnjNlU3QTd6OUm=
A549 MmnHSpVv[3Srb36gRZN{[Xl? Ml3LN{DPxE1? MXe4JIg> Mm\qZoxw[2u|IH3UU3JEOSxiYX7kJGVTUy2PQWDLJIFkfGm4YYTpc44h[2:vYnnu[YQhf2m2aDDNSWsuOTZ{ NHPETHkzPTZ7N{i5PS=>
H460 Mmj4SpVv[3Srb36gRZN{[Xl? NH3pPHY{KM7:TR?= NUO0OG1ZQCCq NFnKeVljdG:la4OgcXRQWkNzLDDhcoQhTVKNLV3BVGsh[WO2aY\heIlwdiClb33ibY5m\CC5aYToJG1GUy1zNkK= MVqyOVY6Pzh7OR?=
RMG1 MnS5R4VtdCCYaXHibYxqfHliQYPzZZk> MmnXNU0{OCEQvF2= Mk\0O|IhcA>? NHvQUnhl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NH\T[FMzPTVzOUG0PC=>
RMG2 M4\id2NmdGxiVnnhZoltcXS7IFHzd4F6 NXToelJjOS1|MDFOwG0> NEj0XWc4OiCq NVvoPI1E\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NEDlNJAzPTVzOUG0PC=>
KOC7C MVfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M13STlEuOzBizszN NVnafG5IPzJiaB?= NFfIVmdl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MV:yOVUyQTF2OB?=
HAC2 MmTyR4VtdCCYaXHibYxqfHliQYPzZZk> MYqxMVMxKM7:TR?= MkW2O|IhcA>? M1PhN4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MkniNlU2OTlzNEi=
RMG2 NGKwT4hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnHnNU0{OCEQvF2= NW\CO5V[PDhiaB?= M{PnUYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NHL2RnYzPTVzOUG0PC=>
OVISE MoHYR4VtdCCYaXHibYxqfHliQYPzZZk> NEjXSlAyNTNyIN88US=> MmDlOFghcA>? M2frUYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NIjIWpYzPTVzOUG0PC=>
SKOV3 MYrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUWxMVMxKM7:TR?= NH;0TGI1QCCq NEXEWpFl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M3;wU|I2PTF7MUS4
A2780 MlvpR4VtdCCYaXHibYxqfHliQYPzZZk> MUmxMVMxKM7:TR?= NYDjUY1wPDhiaB?= NIjSVWtl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MUGyOVUyQTF2OB?=
RMG1 MVXBdI9xfG:|aYOgRZN{e2G7 NWm1elUyOzBizszN NVj5fopHOjRiaB?= MXvpcoR2[2W|IHHwc5B1d3Orcx?= MX[yOVUyQTF2OB?=
RMG2 MWjBdI9xfG:|aYOgRZN{e2G7 Moj0N|Ah|ryP NX7tW2I3OjRiaB?= M1y3Rolv\HWlZYOgZZBweHSxc3nz M4PwXVI2PTF7MUS4
HCC1806 NF3YXZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYmwMVExKM7:TR?= NWXFblJxPDhiaB?= M{GwbmVEPTB;Mj64OQKBkcLz4pEJNE4xPyEQvF2= NIGwUGgzPTJ7M{W3Oi=>
MDA-MB-231  NFfnNmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjibmpqOC1zMDFOwG0> NIexSJQ1QCCq NV;zVYhKTUN3ME2xMlE{6oDLwsJihKkxNjB5IN88US=> MUOyOVI6OzV5Nh?=
GL-1 NHq5N|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3UPWhFOC5z4pETNVAx6oDLzszN MknUOFghcA>? MYnJR|UxRTlwOUGg{txO NH\SVJozPDh6MUWwPC=>
CLBL-1 NGq3VYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXKwMlHjiJNzMEFihKnPxE1? MlP2OFghcA>? NHHjPYpKSzVyPUOzMlAh|ryP NUXCbI5{OjR6OEG1NFg>
UL-1 MlzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXCOXQxNjIkgKOxNFDjiIoQvF2= NF;4RWw1QCCq MVrJR|UxRTdwMEGg{txO NEXjcHAzPDh6MUWwPC=>
Ema M1\odmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPYNE4y6oDVMUCw5qCK|ryP MVy0PEBp M4HqXmlEPTB;NUiuO{DPxE1? M2W2UVI1QDhzNUC4
PANC-1 NGTiNHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnjPZYxNTJ3IN88US=> NUfIS5hjPzJiaB?= NVTuXpZncW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MV6yOFUyQTd3MR?=
MIA MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfMXoFzOC1{NTFOwG0> M3r4ZVczKGh? M4C1folvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NFrGNlczPDVzOUe1NS=>
AsPC-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LPd|AuOjVizszN MlPmO|IhcA>? Mlv4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NFfm[nczPDVzOUe1NS=>
PANC-1 MnnQSpVv[3Srb36gRZN{[Xl? M{OwS|AvPSEQvF2= M3\tXFI1KGh? NG\mT4pqdmirYnn0d{BCc3RuIGO2T|EtKGGwZDDFdosyNzJicHjvd5Bpd3K7bHH0bY9vyqB? NH7TNGczPDVzOUe1NS=>
MIA NWDNe3BrTnWwY4Tpc44hSXO|YYm= MoqxNE42KM7:TR?= MlHaNlQhcA>? NFvW[5JqdmirYnn0d{BCc3RuIGO2T|EtKGGwZDDFdosyNzJicHjvd5Bpd3K7bHH0bY9vyqB? NEPiVJIzPDVzOUe1NS=>
AsPC-1 NH7TSoNHfW6ldHnvckBCe3OjeR?= MVmwMlUh|ryP MX2yOEBp NVzBNlU3cW6qaXLpeJMhSWu2LDDTOmsyNCCjbnSgSZJsOS9{IIDoc5NxcG:{eXzheIlwdsLi MkiyNlQ2OTl5NUG=
U87MG NUTqSoFuS2WubDDWbYFjcWyrdImgRZN{[Xl? Mn;TNE0zPSEQvF2= MnqzNlQuQTZiaB?= NFLjNmRl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[m:2aDDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> MlvJNlQxPjV3MkK=
SGC7901  NELZT|lHfW6ldHnvckBCe3OjeR?= NUXwPZVlOC55NT:xNOKh|ryP NHLGRZE1QCCq MY\k[YNz\WG|ZYOgdE1Cc3RiKGPldkA1PzNrLDDwMWdUUzQQsjCoV4VzKDlrLDDhcoQhSy2PWVOgcIV3\Wy|wrC= NW\XXHFQOjN7MUKyOFY>
MGC803  NEnjfmVHfW6ldHnvckBCe3OjeR?= MWiwMlc2NzFywrFOwG0> NVHid|RjPDkEoHi= Ml\h[IVkemWjc3XzJJAuSWu2IDjT[ZIhPDd|KTygdE1IW0t|zsKgLHNmeiB7KTygZY5lKENvTWnDJIxmfmWuc9Mg MXyyN|kyOjJ2Nh?=
TykNu NFfjTmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLKVY0yUUN3ME2zMlUh|ryP MVmyN|g4PzBzMh?=
TykNuR MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljzTWM2OD13LkWg{txO M13RUFI{QDd5MEGy
M41 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rJSmlEPTB;MkSuO{DPxE1? MmrpNlM5PzdyMUK=
M41R M2HOR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7sboVKSzVyPUG5Mlgh|ryP M1H2XFI{QDd5MEGy
OVCAR8 M1e5VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTNzLkGg{txO M3zFV|I{QDd5MEGy
HeyA8 NXTPfFExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDyNGxKSzVyPUK0MlMh|ryP NGGxdZEzOzh5N{CxNi=>
A2780CP M2PR[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLEWXVKSzVyPUeuOkDPxE1? Mof1NlM5PzdyMUK=
OVCAR5 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Wx[WlEPTB;Nj63JO69VQ>? MWWyN|g4PzBzMh?=
A2780S MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[5TWM2OD1zND61JO69VQ>? M2fGW|I{QDd5MEGy
MCAS Mn3WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLGTWM2OD1zMj61JO69VQ>? NU\qTlhxOjN6N{ewNVI>
NCI-H727 M3nJbmNmdGxiVnnhZoltcXS7IFHzd4F6 M3SwV|AuOTByIN88US=> M1juelI1Nzd{IHi= NEnFO|Rl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[m:2aDDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> MnrMNlI1QTl2M{e=
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... 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:
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
Synonyms NSC639966

Bio Calculators

Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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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