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Ricolinostat (ACY-1215) HDAC Inibitore

Name: Ricolinostat (ACY-1215)
Brand: Selleck Chemicals
SKU: S8001
Rating: 5 (71 reviews)

N. Cat.: S8001

Ricolinostat (ACY-1215, Rocilinostat) è un inibitore selettivo di HDAC6 con una IC50 di 5 nM in un saggio privo di cellule. È >10 volte più selettivo per HDAC6 rispetto a HDAC1/2/3 (HDAC di classe I) con una leggera attività contro HDAC8, attività minima contro HDAC4/5/7/9/11, Sirtuin1 e Sirtuin2. Ricolinostat (ACY-1215) sopprime la proliferazione cellulare e promuove l'apoptosi. Fase 2.

Ricolinostat (ACY-1215) HDAC Inibitore Chemical Structure

Struttura chimica

Peso molecolare: 433.5

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.96%

99.96

Prodotti spesso usati con Ricolinostat (ACY-1215)

(+)-JQ1

It and JQ1 increase apoptosis, diminish the expression of c-MYC and BCL-2, and lower multiple myeloma cells proliferation.

Target correlati	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Sirtuin
Altro HDAC Inibitori	ITF-2357 (Givinostat) Hydrochloride Monohydrate Fimepinostat (CUDC-907) Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A Hydrochloride Tubastatin A Mocetinostat (MGCD0103) 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
A-172	Growth Inhibition Assay	10 nM	24/48 h	inhibits cell growth time dependently	26150340
U87MG	Growth Inhibition Assay	10 nM	24/48 h	inhibits cell growth time dependently	26150340
Hbl-1	Growth Inhibition Assay		48 h	IC50=1.6 μM	26116270
OCI-Ly10	Growth Inhibition Assay		48 h	IC50=0.9 μM	26116270
Riva	Growth Inhibition Assay		48 h	IC50=2.2 μM	26116270
Su-DHL2	Growth Inhibition Assay		48 h	IC50=3.3 μM	26116270
OCI-Ly1	Growth Inhibition Assay		48 h	IC50=2.4 μM	26116270
OCI-Ly7	Growth Inhibition Assay		48 h	IC50=1.2 μM	26116270
Su-DHL4	Growth Inhibition Assay		48 h	IC50=4.7 μM	26116270
Su-DHL6	Growth Inhibition Assay		48 h	IC50=3.2 μM	26116270
Hbl-2	Growth Inhibition Assay		48 h	IC50=1.9 μM	26116270
Jeko-1	Growth Inhibition Assay		48 h	IC50=1.5 μM	26116270
Jvm-2	Growth Inhibition Assay		48 h	IC50=4.0 μM	26116270
Rec-1	Growth Inhibition Assay		48 h	IC50=2.3 μM	26116270
CCL-119	Growth Inhibition Assay		48 h	IC50=1.7 μM	26116270
H9	Growth Inhibition Assay		48 h	IC50=1.2 μM	26116270
HH	Growth Inhibition Assay		48 h	IC50=2.5 μM	26116270
Sup-T1	Growth Inhibition Assay		48 h	IC50=1.6 μM	26116270
MM.1S	Function Assay	0-5μM	6 h	increases acetylated α-tubulin	22262760
MM.1S	Function Assay	0.25/1μM	18 h	increases acetylated α-tubulin	22262760
MM.1R	Function Assay	0.25/1μM	18 h	increases acetylated α-tubulin	22262760
RPMI8226	Function Assay	0.25/1μM	18 h	increases acetylated α-tubulin	22262760
MM.1S	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
OPM1	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
RPMI	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
MM.1R	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
LR5	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
OPM2	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
Sf9	Function assay		10 mins	Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins, IC50 = 0.0047 μM.	28038324
Sf9	Function assay		15 mins	Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay, IC50 = 0.009 μM.	29500130
Sf9	Function assay		15 mins	Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate additi, IC50 = 0.037 μM.	29500130
Sf9	Function assay		10 mins	Inhibition of full length human recombinant C-terminal FLAG-tagged HDAC2 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins, IC50 = 0.048 μM.	28038324
Sf9	Function assay		10 mins	Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins, IC50 = 0.058 μM.	28038324
Sf9	Function assay		15 mins	Inhibition of full length recombinant human C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay, IC50 = 0.066 μM.	29500130
Sf9	Function assay		15 mins	Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence ass, IC50 = 0.1 μM.	29500130
BCP-ALL	Cytotoxicity assay		72 hrs	Cytotoxicity against human BCP-ALL cells derived from patient 1 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 0.29 μM.	30365892
BCP-ALL	Cytotoxicity assay		72 hrs	Cytotoxicity against human BCP-ALL cells derived from patient 4 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 0.54 μM.	30365892
BCP-ALL	Cytotoxicity assay		72 hrs	Cytotoxicity against human BCP-ALL cells derived from patient 2 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 0.58 μM.	30365892
RPMI8226	Cytotoxicity assay		72 hrs	Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay, IC50 = 1.468 μM.	26443078
SEM	Cytotoxicity assay		72 hrs	Cytotoxicity against human SEM cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 1.61 μM.	30365892
SUP-B15	Cytotoxicity assay		72 hrs	Cytotoxicity against human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 1.92 μM.	30365892
RPMI18226	Cytotoxicity assay		72 hrs	Cytotoxicity against human RPMI18226 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 1.97 μM.	30365892
HL60	Cytotoxicity assay		72 hrs	Cytotoxicity against human HL60 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 2.36 μM.	30365892
HL60	Antiproliferative assay		48 hrs	Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM.	29940115
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM.	29940115
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM.	29940115
KCL22	Cytotoxicity assay		72 hrs	Cytotoxicity against imatinib-resistant human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.38 μM.	30365892
U266	Cytotoxicity assay		72 hrs	Cytotoxicity against human U266 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.52 μM.	30365892
SUP-B15	Cytotoxicity assay		72 hrs	Cytotoxicity against imatinib-resistant human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.54 μM.	30365892
KCL22	Cytotoxicity assay		72 hrs	Cytotoxicity against human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.75 μM.	30365892
HL60	Antiproliferative assay		48 hrs	Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM.	29940115
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM.	29940115
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM.	29940115
BCP-ALL	Cytotoxicity assay		72 hrs	Cytotoxicity against human BCP-ALL cells derived from patient 3 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 4.45 μM.	30365892
MV4-11	Function assay	1000 nM	6 hrs	Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as upregulation of histone H3 acetylation at 1000 nM after 6 hrs by Western blot analysis	26443078
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
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
HL60	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human HL60 cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SEM	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human SEM cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SUP-B15	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
HL60	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human HL60 cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SEM	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human SEM cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SUP-B15	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
HL60	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human HL60 cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SEM	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human SEM cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SUP-B15	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SEM	Antiproliferative assay		24 to 72 hrs	Antiproliferative activity against human SEM cells at IC50 to 2 times IC50 after 24 to 72 hrs by trypan exclusion method	30365892
HEL	Cell cycle assay	1 to 10 uM	48 hrs	Cell cycle arrest in human HEL cells assessed as accumulation at G1 phase at 1 to 10 uM after 48 hrs propidium iodide staining based flow cytometry	29940115
SEM	Function assay		18 hrs	Inhibition of HDAC6 in human SEM cells assessed as decrease in aggresome accumulation at IC50 after 18 hrs by fluorescence microscopic method	30365892
SEM	Function assay	1.6 uM	18 hrs	Inhibition of HDAC6 in human SEM cells assessed as decrease in aggresome accumulation at 1.6 uM after 18 hrs by FACS analysis	30365892
SH-SY5Y	Function assay	0.1 to 1 uM	24 hrs	Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in acetylation of alpha-tubulin at 0.1 to 1 uM after 24 hrs by Western blot analysis	30028616
SH-SY5Y	Function assay	0.1 to 1 uM	24 hrs	Inhibition of class 1 HDAC in human SH-SY5Y cells assessed as increase in acetylation of histone H3 at 0.1 to 1 uM after 24 hrs by Western blot analysis	30028616
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	433.5	Formula	C₂₄H₂₇N₅O₃	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	1316214-52-4	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	Rocilinostat			Smiles	C1=CC=C(C=C1)N(C2=CC=CC=C2)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 42 mg/mL (96.88 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.
Clear solution	5%DMSO 1 Corn oil Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	4.000mg/ml (9.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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.
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 (11.53mM)	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.
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.	4.000mg/ml (9.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 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.

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)

Caratteristiche	Induced less cytotoxicity in PHA-stimulated PBMCs from 4 healthy donors compared with the pan-HDAC inhibitor SAHA.
Targets/IC₅₀/Ki	HDAC6 (Cell-free assay) 4.7 nM HDAC2 (Cell-free assay) 48 nM HDAC3 (Cell-free assay) 51 nM HDAC1 (Cell-free assay) 58 nM HDAC8 (Cell-free assay) 100 nM
In vitro	ACY-1215 is a hydroxamic acid derivative. ACY-1215 is 12-, 10-, and 11-fold less active against HDAC1, HDAC2, and HDAC3 (class I HDACs), respectively. ACY-1215 has minimal activity (IC50 > 1μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2, and has slight activity against HDAC8 (IC50 = 0.1μM). The IC50 values for ACY-1215 for T-cell toxicity is 2.5μM. ACY-1215 overcomes tumor cell growth and survival conferred by BMSCs and cytokines in the BM milieu.
Saggio chinasico	Saggi enzimatici HDAC
Saggio chinasico	L'ACY-1215 viene disciolto e successivamente diluito nel tampone di saggio [50 mM HEPES, pH 7,4, 100 mM KCl, 0,001% Tween-20, 0,05% BSA e 20 μM tris(2-carbossietil)fosfina] a 6 volte la concentrazione finale. Gli enzimi HDAC vengono diluiti a 1,5 volte la concentrazione finale nel tampone di saggio e pre-incubati con ACY-1215 per 10 minuti prima dell'aggiunta del substrato. La quantità di FTS (HDAC1, HDAC2, HDAC3 e HDAC6) o MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8 e HDAC9) utilizzata per ciascun enzima è uguale alla costante di Michaelis (Km), come determinata da una curva di titolazione. FTS o MAZ-1675 viene diluito nel tampone di saggio a 6 volte la concentrazione finale con 0,3 μM di tripsina di grado di sequenziamento. La miscela substrato/tripsina viene aggiunta alla miscela enzima/composto e la piastra viene agitata per 60 secondi e quindi posta in un lettore di micropiastre SpectraMax M5. La reazione enzimatica viene monitorata per il rilascio di 7-ammino-4-metossi-cumarina per 30 minuti, dopo la deacetilazione della catena laterale di lisina nel substrato peptidico, e viene calcolata la velocità lineare della reazione.
In vivo	ACY-1215 is readily absorbed by tumor tissue. Moreover, the drug does not accumulate in tumor tissue, as evidenced by the parallel decline of acetylated α-tubulin in blood cells and tumor tissue by 24 hours after dose.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/22262760/

Applicazioni (Applications)

Metodi	Biomarcatori	PMID
Western blot	Ac-α-tubulin / Ac-Histone H4 Survivin / P21 / CDC2 / p53 / p-p53(S392) / Cyclin A2 / Cyclin B1 Bax / Bim / Bcl2 / Cleaved caspase-3 / Cleaved caspase-9 / Cleaved PARP PI3K(p85) / AKT / p-AKT(S473) / PRAS40 / Rag C / mTOR / p-mTOR / ERK / p-ERK Ac-β-catenin(K49) / p-β-catenin / β-catenin	31015208
Immunofluorescence	β-tubulin / β-catenin	25546293
Growth inhibition assay	Cell viability	31015208

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
NCT02632071	Completed	Metastatic Breast Cancer\|Breast Carcinoma	Columbia University\|Acetylon Pharmaceuticals Incorporated\|National Cancer Institute (NCI)	March 1 2016	Phase 1
NCT01583283	Completed	Multiple Myeloma	Celgene	July 12 2012	Phase 1
NCT01323751	Completed	Multiple Myeloma	Celgene\|The Leukemia and Lymphoma Society	July 2011	Phase 1\|Phase 2

Domande Frequenti (Frequently Asked Questions)

Domanda 1:
What would you suggest to obtain a clear solution of it?

Risposta:
It can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 5 mg/ml clearly, while in 1% DMSO/30% polyethylene glycol/1% Tween 80 at 30 mg/ml it is a suspension for oral administration. Please note that the precipitation will go out from the clear solution after stayed for about half an hour, so it is recommended to prepare the solution just before use.

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):