Home Cell Cycle CDK inhibitor Flavopiridol (Alvocidib) HCl

nur für Forschungszwecke

Flavopiridol (Alvocidib) HCl CDK inhibitor

Kat.-Nr.: S2679

Flavopiridol (Alvocidib) HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.
Flavopiridol (Alvocidib) HCl CDK inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 438.3

Springe zu

Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.44%
99.44

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
MCF-7 tumor cell Proliferation assay Inhibition of MCF-7 tumor cell proliferation 10843211
Mia PaCa-2 cell Function assay Inhibition of Mia PaCa-2 cell clonogenic assay, IC50=36 μM 11063609
A2780 cell Function assay Inhibition of A2780 cell clonogenic assay， IC50=15 μM 11063609
HCT116 cell Function assay Inhibition of HCT116 cell clonogenic assay, IC50=13 μM 11063609
PC3 cell Function assay Inhibition of PC3 cell clonogenic assay, IC50=10 μM 11063609
K562 human leukemia cell Proliferation assay Inhibition of K562 human leukemia cell proliferation, IC50=0.13 μM 12190313
MIP human colon carcinoma cell Function assay Inhibition of MIP human colon carcinoma cell line, IC50=0.12 μM 12190313
A549 human lung carcinoma cell Proliferation assay Inhibition of A549 human lung carcinoma cell proliferation, IC50=96 nM 12190313
CACO-2 human colon carcinoma cell Proliferation assay Inhibition of CACO-2 human colon carcinoma cell proliferation, IC50=86 nM 12190313
M109 mouse lung carcinoma cell Proliferation assay Inhibition of M109 mouse lung carcinoma cell proliferation, IC50=80 nM 12190313
A2780/TAX-R human ovarian carcinoma cell Proliferation assay Inhibition of A2780/TAX-R human ovarian carcinoma cell proliferation, IC50=78 nM 12190313
SKBR-3 human breast carcinoma cell Proliferation assay Inhibition of SKBR-3 human breast carcinoma cell proliferation, IC50=77 nM 12190313
A431 human squamous cell Proliferation assay Inhibition of A431 human squamous cell carcinoma cell proliferation, IC50=75 nM 12190313
LX-1 human lung carcinoma Proliferation assay Inhibition of LX-1 human lung carcinoma proliferation, IC50=75 nM 12190313
MLF mouse lung fibroblast cell Proliferation assay Inhibition of MLF mouse lung fibroblast cell proliferation, IC50=72 nM 12190313
PC3 human prostate carcinoma cell Proliferation assay Inhibition of PC3 human prostate carcinoma cell proliferation, IC50=66 nM 12190313
MCF-7 human breast carcinoma cell Proliferation assay Inhibition of MCF-7 human breast carcinoma cell proliferation, IC50=66 nM 12190313
LS174T human colon carcinoma cell Proliferation assay Inhibition of LS174T human colon carcinoma cell proliferation, IC50=65 nM 12190313
A2780/TAX-S human ovarian carcinoma cell Proliferation assay Inhibition of A2780/TAX-S human ovarian carcinoma cell proliferation, IC50=65 nM 12190313
A2780/DDP-S human ovarian carcinoma cell Proliferation assay Inhibition of A2780/DDP-S human ovarian carcinoma cell proliferation, IC50=56 nM 12190313
OVCAR-3 human ovarian carcinoma cell Proliferation assay Inhibition of OVCAR-3 human ovarian carcinoma cell proliferation, IC50=54 nM 12190313
CCRF-CEM human leukemia cell Proliferation assay Inhibition of CCRF-CEM human leukemia cell proliferation, IC50=52 nM 12190313
Hs 27 human fibroblast cell Proliferation assay Inhibition of Hs 27 human fibroblast cell proliferation, IC50=51 nM 12190313
HL60 human leukemia cell Proliferation assay Inhibition of HL60 human leukemia cell proliferation, IC50=46 nM 12190313
ABAE human fibroblast cell Proliferation assay Inhibition of ABAE human fibroblast cell proliferation, IC50=45 nM 12190313
A2780/DDP-R human ovarian carcinoma cell Proliferation assay Inhibition of A2780/DDP-R human ovarian carcinoma cell proliferation, IC50=38 nM 12190313
HCT116/VM46 human colon carcinoma cell Proliferation assay Inhibition of HCT116/VM46 human colon carcinoma cell proliferation, IC50=21 nM 12190313
HCT116 human colon carcinoma cell Proliferation assay Inhibition of HCT116 human colon carcinoma cell proliferation, IC50=18 nM 12190313
HCT116/VP35 human colon carcinoma cell Proliferation assay Inhibition of HCT116/VP35 human colon carcinoma cell proliferation, IC50=17 nM 12190313
LNCaP human prostate carcinoma cell Proliferation assay Inhibition of LNCaP human prostate carcinoma cell proliferation 12190313
human A2780 cell line Proliferation assay 72 h Antiproliferative effect against human A2780 cell line was determined in a whole cell 72 hr cytotoxicity assay, IC50=71 nM 15027863
human ovarian (A2780) cancer cell Cytotoxic assay Cytotoxic effect on human ovarian (A2780) cancer cell line, IC50=71 nM 15125971
ID8 Antiproliferative activity against Antiproliferative activity against ID8 cells, IC50=0.007μM 17123821
MCF7 Antiproliferative activity against Antiproliferative activity against MCF7 cells, IC50=0.026μM 17123821
Sf9 Inhibition of recombinant cyclin A/CDK2 expressed in Inhibition of recombinant cyclin A/CDK2 expressed in Sf9 cells, IC50=0.012μM 17904366
A2780 Inhibition of cdk-mediated NPM phosphorylation at Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 18469809
A2780 Inhibition of cdk-mediated Rb phosphorylation at 24 hrs Inhibition of cdk-mediated Rb phosphorylation at thr821 in human A2780 cells after 24 hrs 18469809
A2780 Inhibition of cdk-mediated Rb phosphorylation at 24 hrs Inhibition of cdk-mediated Rb phosphorylation at ser807/811 in human A2780 cells after 24 hrs 18469809
A2780 Inhibition of cdk9-mediated RNA pol2 CTD phosphorylation at 24 hrs Inhibition of cdk9-mediated RNA pol2 CTD phosphorylation at ser2 in human A2780 cells after 24 hrs 18469809
A2780 Inhibition of cdk7-mediated RNA pol2 CTD phosphorylation at 24 hrs Inhibition of cdk7-mediated RNA pol2 CTD phosphorylation at ser5 in human A2780 cells after 24 hrs 18469809
A2780 Induction of apoptosis in 24 hrs Induction of apoptosis in human A2780 cells assessed as appearance of Mcl1 protein level after 24 hrs 18469809
NCI60 Antiproliferative activity against 72 hrs Antiproliferative activity against human NCI60 cells after 72 hrs by sulforhodamine B assay, GI50=0.0747μM 21080703
NCI60 Antiproliferative activity against 72 hrs Antiproliferative activity against human NCI60 cells assessed as lethal effect after 72 hrs by sulforhodamine B assay, LC50=0.904μM 21080703
DR-U2OS-GFP Reduction of homologous recombination in 0.1 uM 56 hrs Reduction of homologous recombination in human DR-U2OS-GFP cells expressing I-SceI nuclease assessed as reduction of RAD51 level at 0.1 uM after 56 hrs by immunoblotting 21417417
A2780 Cytotoxicity against 24 hrs Cytotoxicity against human A2780 cells after 24 hrs by MTT assay, GI50=0.023μM 23301767
MRC5 Cytotoxicity against 72 hrs Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, GI50=0.028μM 23301767
A2780 Cytotoxicity against 72 hrs Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, GI50=0.029μM 23301767
A2780 Cytotoxicity against 48 hrs Cytotoxicity against human A2780 cells after 48 hrs by MTT assay, GI50=0.031μM 23301767
MRC5 Cytotoxicity against 48 hrs Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay, GI50=0.039μM 23301767
MRC5 Cytotoxicity against 24 hrs Cytotoxicity against human MRC5 cells after 24 hrs by MTT assay, GI50=0.049μM 23301767
HMEC1 Cytotoxicity against 24 hrs Cytotoxicity against human HMEC1 cells after 24 hrs by MTT assay, GI50=0.061μM 23301767
HMEC1 Cytotoxicity against 48 hrs Cytotoxicity against human HMEC1 cells after 48 hrs by MTT assay, GI50=0.062μM 23301767
HMEC1 Cytotoxicity against 72 hrs Cytotoxicity against human HMEC1 cells after 72 hrs by MTT assay, GI50=0.066μM 23301767
A2780 Inhibition of CDK9 in 24 hrs Inhibition of CDK9 in human A2780 cells assessed as reduction of RNAPII CTD phosphorylation at Ser2 at GI50 concentration after 24 hrs by Western blotting analysis 23301767
A2780 Cell cycle arrest in 24 hrs Cell cycle arrest in human A2780 cells assessed as accumulation at G2/M phase at less than GI50 after 24 hrs by flow cytometric analysis 23301767
A2780 Inhibition of CDK9 in 24 hrs Inhibition of CDK9 in human A2780 cells assessed as downregulation of MCL1 at GI50 to 5XGI50 concentration after 24 hrs by Western blotting analysis 23301767
A2780 Inhibition of CDK9 in 24 hrs Inhibition of CDK9 in human A2780 cells assessed as downregulation of HDM2 at GI50 to 5XGI50 concentration after 24 hrs by Western blotting analysis 23301767
A2780 Induction of apoptosis in 24 hrs Induction of apoptosis in human A2780 cells assessed as induction of PARP cleavage at GI50 to 5XGI50 concentration after 24 hrs by Western blotting analysis 23301767
MT4 Antiviral activity against Antiviral activity against Human immunodeficiency virus 1 NL 4-3 infected in MT4 cells measured on day 4 post infection by p24 assay, EC50=0.015μM 25914804
MT4 Cytotoxicity against Cytotoxicity against human MT4 cells, IC50=0.067μM 25914804
Sf9 Inhibition of CDK2/cyclin E1 (unknown origin) expressed in 15 mins Inhibition of CDK2/cyclin E1 (unknown origin) expressed in Sf9 insect cells using UlightCFFKNIVTPRTPPPSQGK-amide substrate after 15 mins by autoradiography, IC50=0.13μM 25914804
A549 Antiproliferative activity against 3 days Antiproliferative activity against human A549 cells after 3 days by SRB method, GI50=0.14μM 25914804
DU145 Antiproliferative activity against 3 days Antiproliferative activity against human DU145 cells after 3 days by SRB method, GI50=0.15μM 25914804
KB Antiproliferative activity against 3 days Antiproliferative activity against human KB cells after 3 days by SRB method, GI50=0.16μM 25914804
KBVIN Antiproliferative activity against 3 days Antiproliferative activity against human KBVIN cells after 3 days by SRB method, GI50=0.18μM 25914804
HCT116 Antiproliferative activity against 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by Celltiter-Glo reagent based assay in presence of 10% fetal bovine serum, EC50=0.034μM 26985305
HCT116 Antiproliferative activity against 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by Celltiter-Glo reagent based assay in presence of 0.625% fetal bovine serum, EC50=0.059μM 26985305
Sf9 Inhibition of human 10 mins Inhibition of human His6-tagged CDK9/cyclin T1 expressed in baculovirus infected sf9 cells using GST-CTD as substrate after 10 mins in presence of [gamma-32P]ATP by SDS-PAGE analysis, IC50=0.0025μM 27171036
Sf21 Inhibition of recombinant human Inhibition of recombinant human full length C-terminal His6-tagged CDK9/cyclin T1 expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate, IC50=0.011μM 27171036
HeLa Cytotoxicity against 72 hrs Cytotoxicity against human HeLa cells assessed as decrease in cell viability after 72 hrs by MTT assay, CC50=0.12μM 27171036
Sf21 Inhibition of full length human Inhibition of full length human N-terminal His6-tagged CDK6/N-terminal GST-tagged cyclin D3 expressed in sf21 cells using histone H1 substrate, IC50=0.395μM 27171036
Sf21 Inhibition of recombinant human Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide, IC50=0.514μM 27171036
HCT116 Antiproliferative activity against 72 hrs Antiproliferative activity against human HCT116 cells assessed as growth inhibition in presence of 0.625% FBS after 72 hrs, EC50=0.059μM 27326333
HepG2 Antiproliferative activity against 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay, EC50=0.1464μM 29407975
KOPN8 Antiproliferative activity against 72 hrs Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay, EC50=0.1926μM 29407975
SEM Antiproliferative activity against 72 hrs Antiproliferative activity against human SEM cells after 72 hrs by CelTiter-Glo assay, EC50=0.2043μM 29407975
UOCB1 Antiproliferative activity against 72 hrs Antiproliferative activity against human UOCB1 cells after 72 hrs by CelTiter-Glo assay, EC50=0.2084μM 29407975
KOPN8 Induction of apoptosis in 0.5 uM 3 to 24 hrs Induction of apoptosis in human KOPN8 cells assessed as upregulation of cleaved PARP level at 0.5 uM after 3 to 24 hrs by Western blot analysis 29407975
KOPN8 Induction of apoptosis in 0.5 uM 1 hr Induction of apoptosis in human KOPN8 cells assessed as upregulation of cleaved PARP level at 0.5 uM pre-treated with NAC for 1 hr and measured after 3 to 24 hrs by Western blot analysis 29407975
insect cells Inhibition of human 2.5 mins Inhibition of human CDK4/cyclin D1 expressed in insect cells after 2.5 mins by liquid scintillation counting analysis, IC50=0.02μM 30733087
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
Caco-2 Toxicity assay 48 hrs Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay, CC50=0.06μM ChEMBL
Caco-2 Function assay 48 hrs Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging, IC50=0.59μM ChEMBL
Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 438.3 Formel

C21H20ClNO5.HCl

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 131740-09-5 SDF herunterladen Lagerung von Stammlösungen

Synonyme NSC 649890, L86-8275, HMR-1275, DSP-2033 Smiles CN1CCC(C(C1)O)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O.Cl

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 88 mg/mL (200.77 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : 37 mg/mL

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

Wirkmechanismus (Mechanism of Action)

Targets/IC50/Ki
CDK1
(Cell-free assay)
40 nM
CDK2
(Cell-free assay)
40 nM
CDK4
(Cell-free assay)
40 nM
CDK6
(Cell-free assay)
40 nM
CDK7
(Cell-free assay)
300 nM
In vitro
Flavopiridol wurde ursprünglich als Inhibitor des epidermalen Wachstumsfaktor-Rezeptors und der Proteinkinase A identifiziert (IC50 = 21 bzw. 122 μM). Später wurde nachgewiesen, dass Flavopiridol bei physiologisch relevanteren Konzentrationen (IC50 = 66 nM) die Zellproliferation hemmt, als Flavopiridol im Rahmen des National Cancer Institute Development Therapeutics Program an einer Gruppe von 60 menschlichen Tumorzelllinien getestet wurde. Flavopiridol induziert einen G1-Arrest mit Hemmung von CDK2 und CDK4 in menschlichen Brustkarzinomzellen in einer zeit- und konzentrationsabhängigen Weise. Eine Kurzzeitbehandlung mit Flavopiridol (~12 Stunden) induziert Apoptose in hämatopoetischen Zelllinien, einschließlich SUDHL4, SUDHL6 (B-Zell-Linien), Jurkat und MOLT4 (T-Zell-Linien) sowie HL60 (myeloisch). Im Koloniebildungsassay wirkt Flavopiridol als hochpotente zytotoxische Verbindung mit einer mittleren IC70 von 8 ng/mL in 23 menschlichen Tumormodellen. Eine aktuelle Studie zeigt, dass die Behandlung mit Flavopiridol eine substanzielle AKT-Ser473-Phosphorylierung in der menschlichen Glioblastom-Zelllinie T98G induziert.
Kinase-Assay
Rekombinante CDKs Kinase-Reaktionen
Die Aktivitäten von CDKs werden in Mikrotiterplatten wie folgt bestimmt. 40 μg Gst-Rb werden mit unterschiedlichen Mengen an Flavopiridol (Alvocidib) HCl und unmarkiertem ATP gemischt. Die Reaktionen werden dann durch Zugabe eines Ammoniumsulfat-Präzipitats der S100-Fraktion gestartet, die aus Insektenzellen gewonnen wurde, welche rekombinante humane CDKs exprimieren. Die endgültigen Reaktionsbedingungen sind 10 mM MgCl2, 50 mM Tris-HCl (pH 7,5) und 1 mM DTT. Die Endkonzentration von ATP wird entsprechend angepasst. Radiomarkiertes ATP wird als Phosphoryldonor verwendet. Die Reaktion wird nach Zugabe des Enzyms 2,5 Minuten lang bei 30 °C durchgeführt und dann durch Zugabe von EDTA beendet. Das Gst-Rb wird anschließend mit Glutathion-Sepharose eingefangen und die eingebaute Radioaktivität durch Flüssigszintillationszählung bestimmt.
In vivo
Bei der maximal tolerierten Dosis von 10 mg/kg/Tag, die an den Tagen 1-4 und 7-11 p.o. verabreicht wurde, bewirkt Flavopiridol (Alvocidib) HCl eine Tumorregression bei PRXF1337 und eine Tumorstase von 4 Wochen bei PRXF1369. Nach der Behandlung mit 7,5 mg/kg Flavopiridol (Alvocidib) HCl als intravenösem (IV) oder intraperitonealem Bolus an 5 aufeinanderfolgenden Tagen zeigten 11 von 12 subkutanen (s.c.) menschlichen HL-60-Xenotransplantaten im fortgeschrittenen Stadium eine vollständige Regression, und die Tiere blieben mehrere Monate nach einem Behandlungszyklus mit Flavopiridol (Alvocidib) HCl krankheitsfrei. SUDHL-4 s.c.-Lymphome, die mit Flavopiridol (Alvocidib) HCl als 7,5 mg/kg Bolus IV für 5 Tage behandelt wurden, zeigten entweder eine starke (zwei von acht Mäusen) oder eine vollständige (vier von acht Mäusen) Regression, wobei zwei Tiere länger als 60 Tage krankheitsfrei blieben. Die gesamte Wachstumsverzögerung beträgt 73,2%. Die tägliche IV- oder IP-Verabreichung von Flavopiridol (Alvocidib) HCl führt zu Spitzenplasmaspiegeln von etwa 7 µM, gefolgt von einem fortschreitenden Abfall auf etwa 100 nM innerhalb von 8 Stunden.
Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/9815683/
  • [5] https://pubmed.ncbi.nlm.nih.gov/22391209/
  • [6] https://pubmed.ncbi.nlm.nih.gov/9516149/

Anwendungen (Applications)

Methoden Biomarker Bilder PMID
Western blot CDK2 / CDK4 / Cyclin A / p21 / p27 / Rb p-ERK / ERK / p-p38 / p-4EBP1 / 4EBP1 / p-S6 p-RNAPII / p-eIF4E / Mnk1 Cleaved caspase-8 / Cleaved caspase-9 / Cleaved caspase-3
S2679-WB4
24572052
Growth inhibition assay Cell viability
S2679-viability1
31193061

Klinische Studieninformationen (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
NCT00112723 Terminated
Adult Lymphocyte Depletion Hodgkin Lymphoma|Adult Lymphocyte Predominant Hodgkin Lymphoma|Adult Mixed Cellularity Hodgkin Lymphoma|Adult Nodular Sclerosis Hodgkin Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Multiple Myeloma|Splenic Marginal Zone Lymphoma|Stage I Multiple Myeloma|Stage II Multiple Myeloma|Stage III Multiple Myeloma|Waldenström Macroglobulinemia
National Cancer Institute (NCI)
 December 2005 Phase 1|Phase 2
NCT00098371 Terminated
B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia
National Cancer Institute (NCI)
 April 2005 Phase 2
NCT00101231 Terminated
Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Relapsing Chronic Myelogenous Leukemia
National Cancer Institute (NCI)
 October 2004 Phase 1
NCT00058240 Completed
B-cell Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Waldenström Macroglobulinemia
National Cancer Institute (NCI)
 April 2003 Phase 1|Phase 2