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Fimepinostat (CUDC-907) inhibiteur de PI3K/HDAC

Name: Fimepinostat (CUDC-907)
Brand: Selleck Chemicals
SKU: S2759
Rating: 5 (37 reviews)

N° Cat.S2759

Le Fimepinostat (CUDC-907) est un double inhibiteur de PI3K et HDAC ciblant PI3Kα et HDAC1/2/3/10 avec des valeurs d'IC50 de 19 nM et 1,7 nM/5 nM/1,8 nM/2,8 nM, respectivement. Ce composé induit un arrêt du cycle cellulaire et l'apoptosis dans les cellules de cancer du sein. Phase 1.

Fimepinostat (CUDC-907) HDAC inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 508.55

Aller à

Contrôle qualité

Lot : Pureté : 99.98%

99.98

Cibles apparentées	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Autre HDAC Inhibiteurs	ITF-2357 (Givinostat) Hydrochloride Monohydrate Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A HCl Tubastatin A Mocetinostat (MGCD0103) Ricolinostat (ACY-1215) PCI-34051

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Description de lactivité	PMID
human Glioma cells (HF2885)	Cytotoxicity assay		72 h	Cytotoxicity against human Glioma cells (HF2885) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM	26288699
human Glioma cells (HF3013)	Cytotoxicity assay		72 h	Cytotoxicity against human Glioma cells (HF3013) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM	26288699
human Glioma cells (HF2876)	Cytotoxicity assay		72 h	Cytotoxicity against human Glioma cells (HF2876) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM	26288699
human Glioma cells (HF2790)	Cytotoxicity assay		72 h	Cytotoxicity against human Glioma cells (HF2790) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM	26288699
human Glioma cells (HF2476)	Cytotoxicity assay		72 h	Cytotoxicity against human Glioma cells (HF2476) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM	26288699
human Glioma cells (HF2381)	Cytotoxicity assay		72 h	Cytotoxicity against human Glioma cells (HF2381) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM	26288699
human Glioma cells (HF2303)	Cytotoxicity assay		72 h	Cytotoxicity against human Glioma cells (HF2303) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM	26288699
MV4-11	Cytotoxicity assay		24 hrs	Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay, =0.00043μM.	27186676
Sf9	Function assay		15 mins	Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr, =0.0018μM.	27186676
Sf9	Function assay		15 mins	Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay, =0.0028μM.	27186676
Sf9	Function assay		15 mins	Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a, =0.005μM.	27186676
Sf9	Function assay		15 mins	Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence , =0.0054μM.	27186676
A2780S	Cytotoxicity assay		24 hrs	Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay, =0.00615μM.	27186676
HCT116	Cytotoxicity assay		24 hrs	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay, =0.00734μM.	27186676
Sf9	Function assay		60 mins	Inhibition of full length recombinant human N-terminal GST-tagged p110 alpha/untagged p85 alpha expressed in baculovirus infected insect Sf9 cells using PI:3PS as substrate incubated for 60 mins by ADP-Glo luminescence assay, =0.019μM.	27186676
Sf9	Function assay		15 mins	Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a, =0.027μM.	27186676
Sf9	Function assay		2 hrs	Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay, =0.039μM.	27186676
Sf9	Function assay		1 hr	Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay, =0.054μM.	27186676
A2780S	Function assay		6 hrs	Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay, =0.12625μM.	27186676
Sf9	Function assay		15 mins	Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after , =0.191μM.	27186676
A2780S	Function assay		6 hrs	Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay, =0.22175μM.	27186676
Sf9	Function assay		15 mins	Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat, =0.409μM.	27186676
Sf9	Function assay		15 mins	Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu, =0.426μM.	27186676
Sf9	Function assay		15 mins	Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas, =0.554μM.	27186676
Sf9	Function assay		15 mins	Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay, =0.674μM.	27186676
Sf9	Function assay			Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110alpha/untagged p85alpha expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescent assay, =0.019μM.	28494256
Sf9	Function assay			Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110delta/untagged p85alpha expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescent assay, =0.039μM.	28494256
Sf9	Function assay			Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110beta/untagged p85alpha expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescent assay, =0.054μM.	28494256
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
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 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
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
Daoy	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells	29435139
Sf9	Function assay			Inhibition of recombinant human full-length N-terminal GST-tagged p110alpha/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay, =0.019μM.	30418766
Sf9	Function assay			Inhibition of recombinant human full-length N-terminal GST-tagged p110delta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay, =0.039μM.	30418766
Sf9	Function assay			Inhibition of recombinant human full-length N-terminal GST-tagged p110beta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay, =0.054μM.	30418766
Sf9	Function assay		15 mins	Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.00036μM.	31117517
Sf9	Function assay		15 mins	Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.0014μM.	31117517
Sf9	Function assay		15 mins	Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.0016μM.	31117517
HCT116	Antiproliferative assay		96 hrs	Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay, =0.005μM.	31117517
HCT8	Antiproliferative assay		96 hrs	Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay, =0.005μM.	31117517
U87	Antiproliferative assay		96 hrs	Antiproliferative activity against human U87 cells after 96 hrs by MTT assay, =0.007μM.	31117517
Capan2	Antiproliferative assay		96 hrs	Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay, =0.007μM.	31117517
MDA-MB-453	Antiproliferative assay		96 hrs	Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay, =0.009μM.	31117517
Bel7402	Antiproliferative assay		96 hrs	Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay, =0.013μM.	31117517
HepG2	Antiproliferative assay		96 hrs	Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay, =0.015μM.	31117517
NCI-H1299	Antiproliferative assay		96 hrs	Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay, =0.025μM.	31117517
MCF7	Antiproliferative assay		96 hrs	Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay, =0.041μM.	31117517
HGC27	Antiproliferative assay		96 hrs	Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay, =0.041μM.	31117517
Sf9	Function assay		15 mins	Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.132μM.	31117517
NCI-H460	Antiproliferative assay		96 hrs	Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay, =0.15μM.	31117517
SW1990	Antiproliferative assay		96 hrs	Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay, =0.18μM.	31117517
K562	Antiproliferative assay		96 hrs	Antiproliferative activity against human K562 cells after 96 hrs by MTT assay, =0.28μM.	31117517
Sf9	Function assay		15 mins	Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.445μM.	31117517
DU145	Antiproliferative assay		96 hrs	Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay, =0.56μM.	31117517
HuH7	Antiproliferative assay		96 hrs	Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay, =0.56μM.	31117517
MV4-11	Antiproliferative assay	25 to 50 nM	72 hrs	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability at 25 to 50 nM after 72 hrs by tryphan blue assay	32212730
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Informations chimiques, stockage et stabilité

Poids moléculaire	508.55	Formule	C₂₃H₂₄N₈O₄S	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	1339928-25-4	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	N/A			Smiles	CN(CC1=CC2=C(S1)C(=NC(=N2)C3=CN=C(C=C3)OC)N4CCOCC4)C5=NC=C(C=N5)C(=O)NO

Solubilité

In vitro
Lot:

DMSO : 102 mg/mL (200.57 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	5.000mg/ml (9.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC₅₀/Ki	HDAC1 (Cell-free assay) 1.7 nM HDAC3 (Cell-free assay) 1.8 nM HDAC10 (Cell-free assay) 2.8 nM HDAC2 (Cell-free assay) 5.0 nM HDAC11 (Cell-free assay) 5.4 nM PI3Kα (Cell-free assay) 19 nM HDAC6 (Cell-free assay) 27 nM PI3Kδ (Cell-free assay) 39 nM PI3Kβ (Cell-free assay) 54 nM
In vitro	Le Fimepinostat (CUDC-907) inhibe d'autres isoformes de PI3K telles que PI3Kβ, PI3Kγ, PI3Kδ, PI3KɑH1047R et PI3KɑE545K avec une IC50 de 54 nM, 311 nM, 39 nM, 73 nM et 62 nM, respectivement. De plus, il prévient également les sous-types de HDAC HDAC8, HDAC6 et HDAC11 avec une IC50 de 191 nM, 27 nM et 5,4 nM, respectivement. En outre, ce composé supprime d'autres types d'activité enzymatique des HDAC avec une puissance inférieure. Il inhibe la croissance d'une série de lymphomes à cellules B tels que Granta 519, DOHH2, RL, Pfeiffer, SuDHL4, Daudi et Raji avec une IC50 de 7 nM, 1 nM, 2 nM, 4 nM, 3 nM, 15 nM et 9 nM, respectivement. Il bloque également la prolifération du myélome, y compris RPMI8226, OPM-2 et ARH77, avec une IC50 de 2 nM, 1 nM et 5 nM, respectivement. Le Fimepinostat présente une activité antitumorale plus importante dans le myélome multiple et le lymphome à cellules B.
In vivo	Le Fimepinostat (CUDC-907) a une longue demi-vie dans les tumeurs murines et induit l'apoptosis tout en inhibant la prolifération des cellules cancéreuses dans les tumeurs xénogreffées. Dans les études d'efficacité sur les modèles de LNH et de MM, ce composé est plus efficace qu'un composé de référence inhibiteur de PI3K ou de HDAC seul ou une combinaison des deux agents administrés à des doses maximales tolérées (DMT). En outre, il est plus efficace que l'inhibiteur sélectif de PI3Kδ CAL-101 lorsqu'il est administré à des doses DMT.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/22693356/

Applications

Méthodes	Biomarqueurs	PMID
Western blot	AKT / p-AKT / P-p70S6K1 / Ac-H3K9 / p-MEK / p-ERK / p-STAT3 / MCL-1 / Bcl-2 / Bcl-xl / PARP p-PRAS40 / p-4EBP1 / p-S6 / c-Myc / Cleaved PARP / Caspase-3 / Celaved caspase-3 SYK / BTK / Bcl-10 / MyD88 / IRAK4	30353642
Immunofluorescence	γ-H2AX / 53BP1 RAD51	29760046
Growth inhibition assay	Cell viability	28147336

Informations sur lessai clinique

(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Sponsor/Collaborateurs	Date de début	Phases
NCT02909777	Active not recruiting	Lymphoma\|Neuroblastoma\|Brain Tumor\|Solid Tumor	Dana-Farber Cancer Institute\|Curis Inc.	October 2016	Phase 1
NCT02307240	Completed	Triple-Negative Breast Cancer\|High-grade Serous Ovarian Cancer\|Solid Tumors\|NUT Midline Carcinoma	Curis Inc.	November 2014	Phase 1
NCT01742988	Completed	Lymphoma\|Relapsed Lymphoma\|Refractory Lymphoma\|Relapsed and/or Refractory Lymphoma\|Relapsed Ddiffuse Large B-Cell Lymphoma (DLBCL)\|Refractory Diffuse Large B-Cell Lymphoma (DLBCL)\|Relapsed and/or Refractory Diffuse Large B-Cell Lymphoma (DLBCL)\|Double-hit Lymphoma (DHL)\|Triple-hit Lymphoma (THL)\|Double-expressor Lymphoma (DEL)\|High-grade B-cell Lymphoma (HGBL)	Curis Inc.\|The Leukemia and Lymphoma Society	December 2012	Phase 1

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

Questions fréquemment posées

Question 1:
How to solve it for in vivo studies (p.o.)?

Réponse :
If you decide to take P.O. as your administration route, we suggest using 1% CMC-Na to dilute it as a suspension solution for gavage.

Question 2:
What is its half-life in vivo?

Réponse :
It is said to have a long half-life in mouse tumor model: http://cancerres.aacrjournals.org/content/72/8_Supplement/3744.short, however, its not formally published and we have no detail of how long it is.

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