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Perifosine Akt Inhibidor

Cat. No.S1037

La Perifosine es un nuevo inhibidor de Akt con una IC50 de 4,7 μM en células MM.1S, que se dirige al dominio de homología de pleckstrina de Akt. Fase 3.
Perifosine Akt Inhibidor Chemical Structure

Estructura química

Peso molecular: 461.66

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Control de calidad (Quality Control)

Lote: Pureza: >97%
97

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad 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
Haga clic para ver más datos experimentales de líneas celulares

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 461.66 Fórmula

C25H52NO4P

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 157716-52-4 Descargar SDF Almacenamiento de soluciones madre

Sinónimos KRX-0401, NSC639966, D21266 Smiles CCCCCCCCCCCCCCCCCCOP(=O)([O-])OC1CC[N+](CC1)(C)C

Solubilidad (Solubility)

In vitro
Lote:

Water : 92 mg/mL

Ethanol : 92 mg/mL

DMSO : Insoluble
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC50/Ki
Akt
(MM.1S cells)
4.7 μM
In vitro

Perifosina desarrolla propiedades antiproliferativas con una IC50 de 0,6-8,9 μM en queratinocitos inmortalizados (HaCaT), y células de carcinoma escamoso de cabeza y cuello. Este compuesto reduce fuertemente los niveles de fosforilación de Akt y de la quinasa regulada por señal extracelular (Erk) 1/2, induce la detención del ciclo celular en G1 y G2, y causa una inhibición del crecimiento dosis-dependiente de los progenitores gliales de ratón. Inhibe completamente la fosforilación de Akt en células MM.1S. Un estudio reciente demuestra que este compuesto químico induce la detención del ciclo celular y la apoptosis en líneas celulares de carcinoma hepatocelular humano mediante el bloqueo de la fosforilación de Akt.

Ensayo de quinasa
Ensayo de quinasa Akt
Las células MM.1S se cultivan en presencia o ausencia de perifosina (5 μM, 6 horas) y luego se estimulan con IL-6 (20 ng/mL, 10 minutos). A continuación, se realiza un ensayo de quinasa Akt in vitro utilizando el kit de ensayo de quinasa Akt.
In vivo

La Perifosina en combinación reduce la proliferación tumoral (una gliomagénesis impulsada por PDGF) in vivo. Los resultados indican que este compuesto es un fármaco eficaz en gliomas en los que las vías Akt y Ras-Erk 1/2 están frecuentemente activadas, y puede ser un nuevo candidato para el tratamiento del glioma en la clínica. Tanto la administración oral diaria como semanal de este químico reducen significativamente el crecimiento tumoral del MM humano y aumentan la supervivencia, en comparación con los animales de control tratados solo con el vehículo PBS. Induce trombocitosis y leucocitosis y aumenta la mielopoyesis en la médula y el bazo murinos, mientras que causa apoptosis en los xenoinjertos de mieloma.

Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/20842425/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17588472/

Aplicaciones (Applications)

Métodos Biomarcadores Imágenes 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
S1037-WB1
25519148
Growth inhibition assay Cell viability
S1037-viability1
28332584

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT Reclutamiento Condiciones Patrocinador/Colaboradores Fecha de inicio Fases
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