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Ricolinostat (ACY-1215) HDAC inhibitor

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

Cat. No.: S8001

Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2.

Ricolinostat (ACY-1215) HDAC inhibitor Chemical Structure

Estructura química

Peso molecular: 433.5

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.96%

99.96

Productos que se suelen utilizar junto 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.

Dianas relacionadas	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Sirtuin
Otros HDAC Inhibidores	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

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	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
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	433.5	Fórmula	C₂₄H₂₇N₅O₃	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	1316214-52-4	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	Rocilinostat			Smiles	C1=CC=C(C=C1)N(C2=CC=CC=C2)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 42 mg/mL (96.88 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Características	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.
Ensayo de quinasa	Ensayos enzimáticos de HDAC
Ensayo de quinasa	ACY-1215 se disuelve y se diluye posteriormente en tampón de ensayo [50 mM HEPES, pH 7,4, 100 mM KCl, 0,001 % Tween-20, 0,05 % BSA y 20 μM tris(2-carboxietil)fosfina] a 6 veces la concentración final. Las enzimas HDAC se diluyen a 1,5 veces la concentración final en tampón de ensayo y se preincuban con ACY-1215 durante 10 minutos antes de la adición del sustrato. La cantidad de FTS (HDAC1, HDAC2, HDAC3 y HDAC6) o MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8 y HDAC9) utilizada para cada enzima es igual a la constante de Michaelis (Km), según lo determinado por una curva de titulación. FTS o MAZ-1675 se diluye en tampón de ensayo a 6 veces la concentración final con 0,3 μM de tripsina de grado de secuenciación. La mezcla de sustrato/tripsina se añade a la mezcla de enzima/compuesto y la placa se agita durante 60 segundos y luego se coloca en un lector de microplacas SpectraMax M5. La reacción enzimática se monitoriza para la liberación de 7-amino-4-metoxi-cumarina durante 30 minutos, después de la desacetilación de la cadena lateral de lisina en el sustrato peptídico, y se calcula la velocidad lineal de la reacción.
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.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/22262760/

Aplicaciones (Applications)

Métodos	Biomarcadores	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

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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

Preguntas frecuentes (Frequently Asked Questions)

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

Respuesta:
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):