uitsluitend voor onderzoeksdoeleinden
Cat.Nr.S1037
| Gerelateerde doelwitten | PI3K mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK |
|---|---|
| Overige Akt Inhibitoren | SC79 AZD5363 (Capivasertib) MK-2206 Dihydrochloride Ipatasertib (GDC-0068) GSK690693 Triciribine (API-2) Afuresertib (GSK2110183) CCT128930 A-674563 HCl Akti-1/2 |
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | 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 | |||
| Klik om meer experimentele gegevens over de cellijn te bekijken | ||||||
| Moleculair gewicht | 461.66 | Formule | C25H52NO4P |
Opslag (Vanaf de ontvangstdatum) | |
|---|---|---|---|---|---|
| CAS-nr. | 157716-52-4 | SDF downloaden | Opslag van stamoplossingen |
|
|
| Synoniemen | 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 |
|||||
Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)
Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH2O, mengen en helder maken.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.
Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
| Targets/IC50/Ki |
Akt
(MM.1S cells) 4.7 μM
|
|---|---|
| In vitro |
Perifosine ontwikkelt antiproliferatieve eigenschappen met een IC50 van 0,6-8,9 μM in geïmmortaliseerde keratinocyten (HaCaT) en plaveiselcarcinoomcellen van hoofd en hals. Deze verbinding vermindert sterk de fosforyleringsniveaus van Akt en extracellulair signaal-gereguleerde kinase (Erk) 1/2, induceert celcyclusarrest in G1 en G2, en veroorzaakt dosisafhankelijke groeiremming van muizengliacellen. Het remt volledig de fosforylering van Akt in MM.1S-cellen. Een recente studie toont aan dat deze chemische stof celcyclusarrest en apoptose induceert in menselijke hepatocellulaire carcinoomcellijnen door blokkade van Akt-fosforylering. |
| Kinase Assay |
Akt kinase test
|
|
MM.1S-cellen worden gekweekt in de aanwezigheid of afwezigheid van perifosine (5 μM, 6 uur) en vervolgens gestimuleerd met IL-6 (20 ng/mL, 10 minuten). In vitro Akt kinase test wordt vervolgens uitgevoerd met behulp van de Akt Kinase Assay Kit.
|
|
| In vivo |
Perifosine in combinatie vermindert de tumorgroei (een PDGF-gedreven gliomagenese) in vivo. De resultaten geven aan dat deze verbinding een effectief medicijn is bij gliomen waarin Akt- en Ras-Erk 1/2-routes frequent geactiveerd zijn, en een nieuwe kandidaat kan zijn voor glioombehandeling in de kliniek. Zowel orale dagelijkse als wekelijkse toediening van deze chemische stof vermindert significant de groei van humane MM-tumoren en verhoogt de overleving, vergeleken met controledieren die alleen met PBS-vehiculum zijn behandeld. Het induceert trombocytose en leukocytose en verhoogt de myelopoëse in het beenmerg en de milt van muizen, terwijl het apoptose veroorzaakt in myeloom-xenografts. |
Referenties |
|
| Methoden | Biomarkers | Afbeeldingen | 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 |
(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Rekrutering | Aandoeningen | Sponsor/Medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| 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 |
Tel: +1-832-582-8158 Ext:3
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