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 50 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.

    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.

  •  

    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.

  • 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  Mmf2SpVv[3Srb36gRZN{[Xl? M1\JbVAvPS9zL{KuOUDPxE1? MX6zJIg> NX;sSlN{emWmdXPld{B1cGViYnHzZYwhS0JidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKGyndnXsd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4TKNVI3ODl5OEez
T24 BC  NFnl[HpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWWwMlUwOS9{LkWg{txO NIPMd28zPCCq NVfQdodz\W6qYX7j[ZMhe2:{YX\lcoljNWmwZIXj[YQh[2WubDD2bYFjcWyrdImg[IVkemWjc3W= NHP1XZEzPjB7N{i3Ny=>
T24 BC  MkHpRZBweHSxc3nzJGF{e3OjeR?= NIHJT5czNjVizszN NW\lfXRFOjRiaB?= NGrSd49{\W6|aYTpfoV{KEKFIHPlcIx{KHSxIIPvdoFn\W6rYj3pcoR2[2WmIHHwc5B1d3SrY9Mg NGDZRpkzPjB7N{i3Ny=>
HepG2 NEXiZVZHfW6ldHnvckBCe3OjeR?= NGXpXnozOMLizszN NFThVJMzPMLiaB?= NVfURoZ5eHKxZIXj[ZMh[W5iaX70[Y5{\SCleYTvdIxie22rYzD2ZYN2d2yrenH0bY9vKGOxcoLld5BwdmSrbnegeI8h[SCwb4ThZoxmKGSrbHH0ZZRqd25ib3[geIhmKEWUIHPpd5Rmem6| NYXIZVB5OjV7M{SyN|I>
U-87 MG  NEfVSohHfW6ldHnvckBCe3OjeR?= M3znWFIxyqEQvF2= M1XVbVI1yqCq NVnBbm5DcW6lcnXhd4V{KGSxdXLs[U1u\W2kcnHu[UBjd3WwZDDzeJJ2[3S3cnXz MUKyOVk{PDJ|Mh?=
HepG2 NEnpTZBHfW6ldHnvckBCe3OjeR?= NVHZe4M{OjEEoN88US=> M3LyZlYwOjRiaB?= MkXmbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZiTFOzMWlKKGOxdILlZZRm\CC5aYToJGNS NX;wOpBmOjV7M{SyN|I>
U-87 MG  MVXGeY5kfGmxbjDBd5NigQ>? NXPzNZJ1OjEEoN88US=> NYLpUIhxPi9{NDDo NWLHNppZcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[gUGM{NUmLIHPveJJm[XSnZDD3bZRpKEOT NFHYVo8zPTl|NEKzNi=>
HepG2 MUfGeY5kfGmxbjDBd5NigQ>? MWOyNOKh|ryP MonSOk8zPCCq NVuyWWNF\GWlcnXhd4V{KEyFMz3JTUBl\We{YXTheIlwdsLiZoLvcUA3KGh? MnnLNlU6OzR{M{K=
U-87 MG  M{\uU2Z2dmO2aX;uJGF{e2G7 M4ezclIxyqEQvF2= M13IN|YwOjRiaB?= MmjHbY5kemWjc3XzJJRp\SCjdYTvdIhi\2mlIH\seZghKGG2IE[gbEB4cGmuZTDpcohq[mm2czD0bIl{KG[udYigZZQhOjSq M1KyT|I2QTN2MkOy
HepG2 NGXUO4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXENlAwPDBizszN M1HOO|I1NzR6IHi= MlXrbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NXG2VoVjOjV7M{SyN|I>
U-87 MG  MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHqc|gzOC92MDFOwG0> NELtbXQzPC92ODDo NGmzNWhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NXO1NmdZOjV7M{SyN|I>
A549 NHf5WplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYWwMlMuOTBizszN MlvzNlQwPzJiaB?= M4rFPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M1LOUVI2Pjl5OEm5
H460 NXzkO|FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnQc4N[OC5|LUGwJO69VQ>? Mn20NlQwPzJiaB?= Mn7IbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MVKyOVY6Pzh7OR?=
A549 Ml\sRZBweHSxc3nzJGF{e3OjeR?= M2H5dlEwOyEQvF2= M3LDfFQ5KGh? M2rwT4lv\HWlZYOgZZBweHSxc3nz M4qzTFI2Pjl5OEm5
H460 Mm\URZBweHSxc3nzJGF{e3OjeR?= MWGxM|Mh|ryP NF;xSZA1QCCq NXnw[Hh1cW6mdXPld{BieG:ydH;zbZM> NVz5TW9ROjV4OUe4PVk>
A549 NGi0O5lHfW6ldHnvckBCe3OjeR?= M3;QOVMh|ryP NFTXS|k5KGh? NUDJT3pb[myxY3vzJGFMXCCjY4TpeoF1cW:w NGjT[YwzPTZ7N{i5PS=>
H460 NUTBO29[TnWwY4Tpc44hSXO|YYm= NF3jNGY{KM7:TR?= NIjHV5g5KGh? MljUZoxw[2u|IFHLWEBi[3SrdnH0bY9v NVHFRm0xOjV4OUe4PVk>
A549 NX\x[I1FTnWwY4Tpc44hSXO|YYm= NHfYTGk{KM7:TR?= M4LySlghcA>? M3Hpb4Jtd2OtczDtWG9TSzFuIHHu[EBGWktvTVHQT{Bi[3SrdnH0bY9vKGOxbXLpcoVlKHerdHigUWVMNTF4Mh?= M2fGZVI2Pjl5OEm5
H460 NH\hNJJHfW6ldHnvckBCe3OjeR?= MYKzJO69VQ>? M1XrflghcA>? Mkn6Zoxw[2u|IH3UU3JEOSxiYX7kJGVTUy2PQWDLJIFkfGm4YYTpc44h[2:vYnnu[YQhf2m2aDDNSWsuOTZ{ NGPkR3MzPTZ7N{i5PS=>
RMG1 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYmxMVMxKM7:TR?= MmrGO|IhcA>? MUXk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MmrnNlU2OTlzNEi=
RMG2 MlHpR4VtdCCYaXHibYxqfHliQYPzZZk> MmLUNU0{OCEQvF2= NYHhNGxjPzJiaB?= M364XYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MWeyOVUyQTF2OB?=
KOC7C NYHWemhpS2WubDDWbYFjcWyrdImgRZN{[Xl? MYexMVMxKM7:TR?= MlTSO|IhcA>? Mojj[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NVzWe25iOjV3MUmxOFg>
HAC2 NXvXcpBTS2WubDDWbYFjcWyrdImgRZN{[Xl? Mm\xNU0{OCEQvF2= MVq3NkBp M4W5ToRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NELBdYEzPTVzOUG0PC=>
RMG2 NXm1eGZKS2WubDDWbYFjcWyrdImgRZN{[Xl? NFLxdoMyNTNyIN88US=> MYK0PEBp NGXvPFNl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MXWyOVUyQTF2OB?=
OVISE NWLNXWJjS2WubDDWbYFjcWyrdImgRZN{[Xl? NH7uV2wyNTNyIN88US=> M4O4VlQ5KGh? M4jOb4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= Ml:zNlU2OTlzNEi=
SKOV3 MUTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFm2UVYyNTNyIN88US=> MmHmOFghcA>? NID0S2pl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NEDqXFAzPTVzOUG0PC=>
A2780 MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NI\uWo8yNTNyIN88US=> NVzNOlJVPDhiaB?= M4Xk[4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NWPFdGZGOjV3MUmxOFg>
RMG1 M3LV[WFxd3C2b4Ppd{BCe3O|YYm= NHX3OGM{OCEQvF2= NETuXo4zPCCq M1TQNIlv\HWlZYOgZZBweHSxc3nz MnLzNlU2OTlzNEi=
RMG2 NEfvNWhCeG:ydH;zbZMhSXO|c3H5 MWCzNEDPxE1? M2fLZlI1KGh? MlTSbY5lfWOnczDhdI9xfG:|aYO= MXGyOVUyQTF2OB?=
HCC1806 NXLP[WpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT4UoYxNTFyIN88US=> MlrVOFghcA>? NWnUc4lnTUN3ME2yMlg16oDLwsJihKkxNjB5IN88US=> NXXJVVBFOjV{OUO1O|Y>
MDA-MB-231  MlWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnGbm5tOC1zMDFOwG0> M2jqVlQ5KGh? M{DB[2VEPTB;MT6xN-KBkcLz4pEJNE4xPyEQvF2= NYmxbHNLOjV{OUO1O|Y>
GL-1 NVPEN2M{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33WdVAvOeLCk{GwNQKBkc7:TR?= NGOwPJE1QCCq NETR[HNKSzVyPUmuPVEh|ryP NWX6RVJYOjR6OEG1NFg>
CLBL-1 NHLKV29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlP4NE4y6oDVMUCw5qCK|ryP M3qzclQ5KGh? M1fufWlEPTB;M{OuNEDPxE1? MUmyOFg5OTVyOB?=
UL-1 NIrnWoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKwMlHjiJNzMEFihKnPxE1? MofEOFghcA>? MWjJR|UxRTdwMEGg{txO MYiyOFg5OTVyOB?=
Ema MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1OyTlAvOeLCk{GwNQKBkc7:TR?= NGDEbHM1QCCq MlHnTWM2OD13OD63JO69VQ>? MUWyOFg5OTVyOB?=
PANC-1 NWj2Z5ZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zDcVAuOjVizszN NGSwcmM4OiCq NFPlcWlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NIjvT|EzPDVzOUe1NS=>
MIA NGCwdYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PSUFAuOjVizszN M33keVczKGh? MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M{nVcFI1PTF7N{Wx
AsPC-1 NIDF[FhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2S3ZVAuOjVizszN NHTneWc4OiCq M{Hy[olvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MXyyOFUyQTd3MR?=
PANC-1 MWjGeY5kfGmxbjDBd5NigQ>? NGG4N|ExNjVizszN NEP0dpUzPCCq NVT3VWE6cW6qaXLpeJMhSWu2LDDTOmsyNCCjbnSgSZJsOS9{IIDoc5NxcG:{eXzheIlwdsLi MlTvNlQ2OTl5NUG=
MIA M3TzPWZ2dmO2aX;uJGF{e2G7 MWOwMlUh|ryP NGPoRnYzPCCq NWnvfI1ucW6qaXLpeJMhSWu2LDDTOmsyNCCjbnSgSZJsOS9{IIDoc5NxcG:{eXzheIlwdsLi NUXyT2lZOjR3MUm3OVE>
AsPC-1 MU\GeY5kfGmxbjDBd5NigQ>? NVvjVmlFOC53IN88US=> NVHCWopKOjRiaB?= MkOxbY5pcWKrdIOgRYt1NCCVNluxMEBidmRiRYLrNU8zKHCqb4PwbI9zgWyjdHnvcuKh NYriWoxnOjR3MUm3OVE>
U87MG MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEG0bFExNTJ3IN88US=> M4K0PVI1NTl4IHi= MkTx[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIJwfGhiZH;z[UBidmRidHnt[UBl\XCnbnTlcpQhdWGwbnXy Ml;6NlQxPjV3MkK=
SGC7901  NVvCNmd6TnWwY4Tpc44hSXO|YYm= MYKwMlc2NzFywrFOwG0> NYHyTnZFPDhiaB?= NV[ybpoy\GWlcnXhd4V{KHBvQXv0JEhU\XJiNEezLUwheC2JU1uz{tIhMFOncjC5LUwh[W6mIFOtUXlEKGyndnXsd:Kh NVT4W2htOjN7MUKyOFY>
MGC803  NFfnNG5HfW6ldHnvckBCe3OjeR?= M13NfVAvPzVxMUFCpO69VQ>? MWO0POKhcA>? NEmwRnRl\WO{ZXHz[ZMheC2Da4SgLHNmeiB2N{OpMEBxNUeVS{ROtkApW2W{IEmpMEBidmRiQz3NXWMhdGW4ZXzzxsA> NVS1RZVPOjN7MUKyOFY>
TykNu M3Xpb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHUTWM2OD1|LkWg{txO MlLGNlM5PzdyMUK=
TykNuR NEjoblBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fHeWlEPTB;NT61JO69VQ>? M4f4TlI{QDd5MEGy
M41 NHvqVWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\3PYhKSzVyPUK0Mlch|ryP NF3Fe5EzOzh5N{CxNi=>
M41R NEHEcm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;xTWM2OD1zOT64JO69VQ>? NVnEeIdmOjN6N{ewNVI>
OVCAR8 MnrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XKcGlEPTB;M{GuNUDPxE1? NEDsdmQzOzh5N{CxNi=>
HeyA8 M1rETGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTJ2LkOg{txO NYTpfXdLOjN6N{ewNVI>
A2780CP Mmn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXWWnBKSzVyPUeuOkDPxE1? MkPUNlM5PzdyMUK=
OVCAR5 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XHXmlEPTB;Nj63JO69VQ>? Ml3xNlM5PzdyMUK=
A2780S NVTPXII2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jWfWlEPTB;MUSuOUDPxE1? MYqyN|g4PzBzMh?=
MCAS M3;NTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTF{LkWg{txO MUiyN|g4PzBzMh?=
NCI-H727 NH\LfnRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3WwRlAuOTByIN88US=> NWfWNFQ5OjRxN{KgbC=> MYHk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZo91cCCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueEBu[W6wZYK= NGnWPHgzOjR7OUSzOy=>
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MAVER MlzsRZBweHSxc3nzJGF{e3OjeR?= MmrWNVDDqM7:TR?= MnzKNlQwPDhiaB?= M2jvWolv\HWlZYOgZZBweHSxc3nzJJRqdWVvZHXw[Y5l\W62bIm= MWiyNFE{ODl4MB?=
BJAB M{TnWWFxd3C2b4Ppd{BCe3O|YYm= NF6xfpYyOMLizszN MYeyOE81QCCq NHvCUY9qdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nLXTldIVv\GWwdHz5 NUHmT2xSOjBzM{C5OlA>
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HL-60 NInGR5dCeG:ydH;zbZMhSXO|c3H5 NVPxVZhwOTEEoN88US=> NWrLbVh5OjRxNEigbC=> Ml\LbY5lfWOnczDhdI9xfG:|aYOgeIlu\S2mZYDlcoRmdnSueR?= M1LocVIxOTNyOU[w

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02238496 Unknown status Brain Tumor Recurrent|Glioblastoma|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Mixed Glioma Andrew Lassman|Pfizer|AEterna Zentaris|Columbia University July 2014 Phase 2
NCT01224730 Completed Cancer AEterna Zentaris January 24 2012 Phase 1
NCT01097018 Completed Colorectal Cancer AEterna Zentaris April 2010 Phase 3
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
NCT01051557 Terminated 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 27 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