nur für Forschungszwecke
Kat.-Nr.: S1037
Chemische Struktur
| Verwandte Ziele | PI3K mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK |
|---|---|
| Weitere Akt Inhibitoren | SC79 AZD5363 (Capivasertib) MK-2206 Dihydrochloride Ipatasertib (GDC-0068) GSK690693 Triciribine (API-2) Afuresertib (GSK2110183) CCT128930 A-674563 HCl AKTi-1/2 (AKT Inhibitor VIII) |
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | 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 | |||
| Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen | ||||||
| Molekulargewicht | 461.66 | Formel | C25H52NO4P |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 157716-52-4 | SDF herunterladen | Lagerung von Stammlösungen |
|
|
| Synonyme | KRX-0401, NSC639966, D21266 | Smiles | CCCCCCCCCCCCCCCCCCOP(=O)([O-])OC1CC[N+](CC1)(C)C | ||
|
In vitro |
Water : 92 mg/mL Ethanol : 92 mg/mL
DMSO
: Insoluble
|
|
In vivo |
|||||
Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)
Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)
Berechnungsergebnisse:
Arbeitskonzentration: mg/ml;
Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.
Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.
| Targets/IC50/Ki |
Akt
(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. This compound 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. It completely inhibits the phosphorylation of Akt in MM.1S cells. A recent study demonstrates this chemical induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation. |
| Kinase-Assay |
Akt-Kinase-Assay
|
|
MM.1S-Zellen werden in An- oder Abwesenheit von Perifosine (5 μM, 6 Stunden) kultiviert und anschließend mit IL-6 (20 ng/mL, 10 Minuten) stimuliert. Ein In-vitro-Akt-Kinase-Assay wird dann unter Verwendung des Akt Kinase Assay Kits durchgeführt.
|
|
| In vivo |
Perifosine in combination reduces tumor proliferation (a PDGF-driven gliomagenesis) in vivo. The results indicate that this compound 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. Both oral daily and weekly administration of this chemical significantly reduce human MM tumor growth and increase survival, compared with control animals treated with PBS vehicle only. It induces thrombocytosis and leukocytosis and increases myelopoiesis in murine marrow and spleen, whereas it causes apoptosis in myeloma xenografts. |
Literatur |
|
| Methoden | Biomarker | Bilder | 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 |
(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)
| NCT-Nummer | Rekrutierung | Erkrankungen | Sponsor/Kooperationspartner | Startdatum | Phasen |
|---|---|---|---|---|---|
| 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 |