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Fimepinostat (CUDC-907) PI3K/HDAC inhibitor

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

N. Cat.: S2759

CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1.

Fimepinostat (CUDC-907) HDAC inhibitor Chemical Structure

Struttura chimica

Peso molecolare: 508.55

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.98%

99.98

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

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dell'attività	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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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	508.55	Formula	C₂₃H₂₄N₈O₄S	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	1339928-25-4	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	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

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 102 mg/mL (200.57 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

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	Fimepinostat (CUDC-907) inibisce altre isoforme di PI3K come PI3Kβ, PI3Kγ, PI3Kδ, PI3KɑH1047R e PI3KɑE545K con IC50 rispettivamente di 54 nM, 311 nM, 39 nM, 73 nM e 62 nM. Inoltre, previene anche i sottotipi di HDAC HDAC8, HDAC6 e HDAC11 con IC50 rispettivamente di 191 nM, 27 nM e 5,4 nM. Inoltre, questo composto sopprime altri tipi di attività enzimatica di HDAC con minore potenza. Inibisce la crescita di una serie di linfomi a cellule B come Granta 519, DOHH2, RL, Pfeiffer, SuDHL4, Daudi e Raji con IC50 rispettivamente di 7 nM, 1 nM, 2 nM, 4 nM, 3 nM, 15 nM e 9 nM. Blocca anche la proliferazione del mieloma, inclusi RPMI8226, OPM-2 e ARH77 con IC50 rispettivamente di 2 nM, 1 nM e 5 nM. Fimepinostat mostra una maggiore attività antitumorale nel mieloma multiplo e nel linfoma a cellule B.
In vivo	Fimepinostat (CUDC-907) ha una lunga emivita nei tumori murini e induce apoptosi inibendo la proliferazione delle cellule tumorali in tumori xenograft. Negli studi di efficacia su modelli di NHL e MM, questo composto è più efficace sia di un composto di riferimento inibitore di PI3K o HDAC a singolo agente, sia di una combinazione dei due agenti somministrati a dosi massimamente tollerate (MTD). Inoltre, è più efficace dell'inibitore selettivo di PI3Kδ CAL-101 quando somministrato a dosi MTD.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/22693356/

Applicazioni (Applications)

Metodi	Biomarcatori	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

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

Domande Frequenti (Frequently Asked Questions)

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

Risposta:
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.

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

Risposta:
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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):