solo para uso en investigación

Belinostat (PXD101) HDAC Inhibidor

Name: Belinostat (PXD101)
Brand: Selleck Chemicals
SKU: S1085
Rating: 5 (106 reviews)

Cat. No.: S1085

Belinostat es un nuevo inhibidor de HDAC con IC50 de 27 nM en un ensayo sin células, con actividad demostrada en tumores resistentes al cisplatino. Belinostat (PXD101) induce autophagy.

Belinostat (PXD101) HDAC Inhibidor Chemical Structure

Estructura química

Peso molecular: 318.35

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.74%

99.74

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) Ricolinostat (ACY-1215)

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

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Formulación	Descripción de la actividad	PMID
HCT116	Function Assay	0.9 μM	24 h		down-regulats TS protein levels after 6 h incubation	17124594
HCT116	Growth Inhibition Assay		48 h		EC50=0.28 μM	17124594
Granta-519	Growth Inhibition Assay		24 h		IC50=56.3 μM	20068080
Jeko-1	Growth Inhibition Assay		24 h		IC50=0.2 μM	20068080
HBL-2	Growth Inhibition Assay		24 h		IC50=0.4 μM	20068080
Panc-1	Apoptosis Assay	100/500/1000 nM	48 h		induces dose dependent apoptosis	22681698
AsPC-1	Apoptosis Assay	100/500/1000 nM	48 h		induces dose dependent apoptosis	22681698
T3M4	Apoptosis Assay	100/500/1000 nM	48 h		induces dose dependent apoptosis	22681698
Panc-1	Growth Inhibition Assay	0-800 nM	48 h		inhibits cell proliferation in a dose dependent manner	22681698
AsPC-1	Growth Inhibition Assay	0-800 nM	48 h		inhibits cell proliferation in a dose dependent manner	22681698
T3M4	Growth Inhibition Assay	0-800 nM	48 h		inhibits cell proliferation in a dose dependent manner	22681698
MiaPaCa2	Function Assay	1/10 μM	24 h		induces growth arrested in G2/M	23475695
AsPc1	Function Assay	1/10 μM	24 h		induces growth arrested in G2/M	23475695
Panc0403	Apoptosis Assay	1 μM	24 h		induces apoptosis	23475695
Panc1005	Apoptosis Assay	1 μM	24 h		induces apoptosis	23475695
Panc0327	Apoptosis Assay	1 μM	24 h		induces apoptosis	23475695
Panc0203	Growth Inhibition Assay		48 h		EC50=22.2 μM	23475695
PL45	Growth Inhibition Assay		48 h		EC50=20.8 μM	23475695
Panc1005	Growth Inhibition Assay		48 h		EC50=1.1 μM	23475695
Panc0403	Growth Inhibition Assay		48 h		EC50=1.1 μM	23475695
BxPc3	Growth Inhibition Assay		48 h		EC50=1.0 μM	23475695
MiaPaCa2	Growth Inhibition Assay		48 h		EC50=0.7 μM	23475695
Panc0327	Growth Inhibition Assay		48 h		EC50=0.5 μM	23475695
AsPc1	Growth Inhibition Assay		48 h		EC50=0.3 μM	23475695
PC9	Function Assay	0.5/1/2 μM	4 h	DMSO	inhibits the levels of Akt (p-Akt) and EGFR	23515752
H1650	Function Assay	0.5/1/2 μM	4 h	DMSO	inhibits the levels of Akt (p-Akt) and EGFR	23515752
H460	Function Assay	0.5/1/2 μM	4 h	DMSO	inhibits the levels of Akt (p-Akt) and EGFR	23515752
PC9	Function Assay	500 nM	24 h	DMSO	decreases EGFR expression	23515752
H1650	Function Assay	500 nM	24 h	DMSO	decreases EGFR expression	23515752
H460	Function Assay	500 nM	24 h	DMSO	decreases EGFR expression	23515752
HCC4006	Growth Inhibition Assay		72 h	DMSO	IC50=0.46 μM	23515752
HCC2935	Growth Inhibition Assay		72 h	DMSO	IC50=0.97 μM	23515752
HCC827	Growth Inhibition Assay		72 h	DMSO	IC50=0.29 μM	23515752
HCC2279	Growth Inhibition Assay		72 h	DMSO	IC50=0.4 μM	23515752
PC9	Growth Inhibition Assay		72 h	DMSO	IC50=0.29 μM	23515752
H820	Growth Inhibition Assay		72 h	DMSO	IC50=0.4 μM	23515752
H1650	Growth Inhibition Assay		72 h	DMSO	IC50=0.88 μM	23515752
H1975	Growth Inhibition Assay		72 h	DMSO	IC50=0.68 μM	23515752
H520	Growth Inhibition Assay		72 h	DMSO	IC50=0.75 μM	23515752
H1299	Growth Inhibition Assay		72 h	DMSO	IC50=1.2 μM	23515752
H460	Growth Inhibition Assay		72 h	DMSO	IC50=0.86 μM	23515752
H1666	Growth Inhibition Assay		72 h	DMSO	IC50>10 μM	23515752
PANC-1	Function Assay	10 μM	2/4 h	DMSO	increases intracellular ROS level	23743198
PANC-1	Cell Viability Assay	1/10 μM	48 h	DMSO	decreases cell viability in a dose dependent manner	23743198
PANC-1	Function Assay	10 μM	2/4/6 h	DMSO	induces AMPK activation	23743198
HL-60	Function Assay	0.2 μM	24/48/72 h		enhances RA-induced granulocytic differentiation	25864732
NB4	Function Assay	0.2 μM	24/48/72 h		enhances RA-induced granulocytic differentiation	25864732
HL-60	Function Assay	2 μM	24/48 h		blocks cell cycle in S phase	25864732
NB4	Function Assay	2 μM	24/48 h		blocks cell cycle in S phase	25864732
HL-60	Cell Viability Assay	0.2/2 μM	24/48/72 h		decreases cell viability in both time and dose dependent manner	25864732
NB4	Cell Viability Assay	0.2/2 μM	24/48/72 h		decreases cell viability in both time and dose dependent manner	25864732
RAW264.7	Anti-inflammatory assay		1 hr		Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method, IC50 = 0.000059 μM.	25113875
HEK293	Function assay				Inhibition of HDAC6 in HEK293 cells, IC50 = 0.015 μM.	18308563
HEK293	Function assay				Inhibition of HDAC1 in HEK293 cells, IC50 = 0.018 μM.	18308563
HeLa	Function assay		30 mins		Inhibition of HDAC in human HeLa cells nuclear extracts incubated for 30 mins by fluorescent assay, IC50 = 0.0264 μM.	25113875
HeLa	Function assay				Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay, IC50 = 0.027 μM.	23639537
HeLa	Function assay				Inhibition of HDAC from human HeLa cells, IC50 = 0.028 μM.	18247554
HEK293	Function assay				Inhibition of HDAC3 in HEK293 cells, IC50 = 0.046 μM.	18308563
MDA-MB-231	Antiproliferative assay		72 hrs		Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.062 μM.	29456804
Jurkat	Antiproliferative assay		48 hrs		Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay, IC50 = 0.07 μM.	29533873
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.077 μM.	29456804
HeLa	Antiproliferative assay		72 hrs		Antiproliferative activity against human HeLa cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.087 μM.	29456804
MCF7	Antiproliferative assay		72 hrs		Antiproliferative activity against human MCF7 cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.096 μM.	29456804
HEL	Antiproliferative assay		48 hrs		Antiproliferative activity against human HEL cells after 48 hrs by MTT assay, IC50 = 0.1 μM.	29533873
Huh7	Antiviral assay		3 days		Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50 = 0.12 μM.	25490700
HCT116	Antiproliferative assay		48 hrs		Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay, GI50 = 0.13 μM.	27344487
MOLT4	Antiproliferative assay		48 hrs		Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay, IC50 = 0.14 μM.	29533873
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50 = 0.16 μM.	21650221
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells, IC50 = 0.16 μM.	21742496
SK-N-BE(2)	Antiproliferative assay		48 hrs		Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay, IC50 = 0.31 μM.	29533873
PC3	Antiproliferative assay		48 hrs		Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay, GI50 = 0.39 μM.	27344487
PC3	Antiproliferative assay		96 hrs		Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay, IC50 = 0.45 μM.	21634430
H1299	Antiproliferative assay				Antiproliferative activity against human H1299 cells, IC50 = 0.46 μM.	21650221
HeLa	Antiproliferative assay		48 hrs		Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.51 μM.	29533873
HCT116	Antiproliferative assay		96 hrs		Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay, IC50 = 0.6 μM.	21634430
A2780	Antiproliferative assay		96 hrs		Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay, IC50 = 0.67 μM.	21634430
HuH7	Cytotoxicity assay		3 days		Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50 = 0.68 μM.	25490700
COLO205	Antiproliferative assay		96 hrs		Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay, IC50 = 0.7 μM.	21634430
A549	Antiproliferative assay		48 hrs		Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, GI50 = 0.78 μM.	27344487
HL60	Antiproliferative assay		48 hrs		Antiproliferative activity against human HL60 cells after 48 hrs by SRB assay, GI50 = 1.09 μM.	27344487
K562	Antiproliferative assay		48 hrs		Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.1 μM.	29533873
PC3	Antiproliferative assay		48 hrs		Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 1.3 μM.	29533873
NFF	Cytotoxicity assay		72 hrs		Cytotoxicity against human NFF cells after 72 hrs by SRB assay, IC50 = 1.4 μM.	28241112
HEK293	Cytotoxicity assay		48 hrs		Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay, IC50 = 1.4 μM.	28241112
NFF	Cytotoxicity assay		72 hrs		Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay, IC50 = 1.42 μM.	30245402
HEK293	Cytotoxicity assay		48 hrs		Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay, IC50 = 1.42 μM.	30245402
RAW264.7	Anti-inflammatory assay		1 hr		Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of nitric oxide production pre-incubated for 1 hr before LPS stimulation for 24 hrs by Griess reagent based assay, IC50 = 2.2 μM.	25113875
RAW264.7	Anti-inflammatory assay		1 hr		Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of TNFalpha production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method, IC50 = 4.7 μM.	25113875
RAW264.7	Anti-inflammatory assay		1 hr		Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of PGE2 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by enzyme immunoassay method, IC50 = 8.28 μM.	25113875
Huh-luc/neo7	Function assay	1 uM	1 to 3 hrs		Inhibition of HDAC class 1 in human Huh-luc/neo7 cells assessed as histone H3 acetylation at 1 uM after 1 to 3 hrs by Western blotting analysis	25937017
PC3	Function assay	0.3 uM	48 hrs		Inhibition of HDAC in human PC3 cells assessed as increase in amount of acetylated histone H3 at 0.3 uM after 48 hrs by Western blot analysis	27344487
HCT116	Function assay	0.3 uM	48 hrs		Inhibition of HDAC in human HCT116 cells assessed as increase in amount of acetylated histone H3 at 0.3 uM after 48 hrs by Western blot analysis	27344487
Haga clic para ver más datos experimentales de líneas celulares

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	318.35	Fórmula	C₁₅H₁₄N₂O₄S	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	866323-14-0	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	PXD101,NSC726630, PX-105684			Smiles	C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)C=CC(=O)NO

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 64 mg/mL (201.03 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.
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.	4.000mg/ml (12.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	1.000mg/ml (3.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 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.

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	Lead compound of Topotarget.
Targets/IC₅₀/Ki	HDAC (Cell-free assay) 27 nM
In vitro	Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells, which are cisplatin and doxorubicin-resistant derivatives of A2780 cells. This compound could induce apoptosis through PARP cleavage and acetylation of histones H3/H4. It inhibits bladder cancer cell growth, especially in 5637 cells, which shows accumulation of G0-G1 phase, decrease in S phase and increase in G2-M phase. The growth inhibitory activity of this chemical on cell lines is not strongly influenced by the multidrug-resistant phenotype, whereas the activity of docetaxel is clearly affected. It could enhance the growth inhibitory activity of docetaxel or carboplatin in OVCAR-3 and A2780 cells. This compound also shows enhanced tubulin acetylation in ovarian cancer cell lines. A recent study shows that it activates protein kinase A in a TGF-β signaling-dependent mechanism and decreases survivin mRNA.
Ensayo de quinasa	Actividad de la Histona Desacetilasa
Ensayo de quinasa	Los cultivos subconfluentes se cosechan y se lavan dos veces en PBS frío y se pelletizan por centrifugación a 200 × g durante 5 min. El pellet celular se resuspende en dos volúmenes de tampón de lisis [tampón Tris 60 mM (pH 7,4) que contiene 30% de glicerol y 450 mM de NaCl] y se lisa mediante tres ciclos de congelación (hielo seco) y descongelación (baño de agua a 30 °C). Los restos celulares se eliminan por centrifugación a 1,2 × 10⁴ g durante 5 min, y el sobrenadante se almacena a −80 °C. El péptido de histona H4 (secuencia SGRGKGGKGLGKGGAKRHRK correspondiente a los 20 residuos NH2-terminales) se acetila mediante una proteína recombinante que contiene el dominio hipoxantina-aminopterina-timidina de p300, utilizando [³H]acetil CoA como fuente de acetato. El péptido H4 (100 μg) se mezcla con tampón de hipoxantina-aminopterina-timidina (50 mM Tris HCl pH 8,0, 5% glicerol, 50 mM KCl y 0,1 mM EDTA), 1 mM DTT, 1 mM 4-(2-aminoetil)bencenosulfonilfluoruro, 1 × inhibidores de proteasa completos, 50 μL de p300 purificada y 1,85 m [³H]acetil CoA (4,50 Ci/mmol) en un volumen final de 300 μL y se incuba a 30 °C durante 45 min. La proteína p300 se elimina por incubación con 20 μL de perlas de Ni-agarosa al 50% durante 1 hora a 4 °C y centrifugación. El sobrenadante se aplica a una columna de Sephadex G15 de 2 mL, y se recoge el flujo pasante. Se aplica suavemente un mililitro de H₂O destilada, y se recogen fracciones de tres gotas; esto se repite hasta que se hayan añadido 4–5 mL de H₂O destilada, y se recogen ~40 fracciones. Tres microlitros de cada fracción se diluyen en 2 mL de líquido de centelleo y se cuentan en un contador de centelleo para identificar las fracciones que contienen el péptido marcado. Estas fracciones se agrupan, y se mide 1 μL de la muestra combinada para evaluar la radioactividad en cada lote de péptido (3-7×10³ cpm/μL). Para los ensayos de actividad, la reacción se lleva a cabo en un volumen total de 150 μL de tampón [60 mM Tris (pH 7,4) que contiene 30% de glicerol] que contiene 2 μL de extracto celular y, cuando se utiliza, 2 μL de este compuesto. La reacción se inicia con la adición de 2 μL de sustrato marcado con [³H] (péptido de histona H4 acetilado correspondiente a los 20 residuos NH₂-terminales). Las muestras se incuban a 37 °C durante 45 min, y la reacción se detiene con la adición de HCl y ácido acético (concentraciones finales de 0,72 y 0,12 M, respectivamente). El [³H]acetato liberado se extrae en 750 μL de acetato de etilo, y las muestras se centrifugan a 1,2 × 10⁴ g durante 5 min. La fase superior (600 μL) se transfiere a 3 mL de líquido de centelleo y se cuenta.
In vivo	Belinostat indicates significant tumor growth delay in A2780 and A2780/cp70 xenograft at a dose of 10mg/kg with no effects on the body weight. This compound also induces p21WAF1, HDAC core and cell communication genes in mouse bladder tumors. Its monotherapy induces dose-proportional antitumor effects with TGI of 47% at a dose of 100mg/kg in A2780 xenograft. The combination of this chemical (100 mg/kg) with carboplatin (40 mg/kg) could delay tumor growth from 18.6 days to 22.5 days. Combining with bortezomib, it results in great tumor inhibition and gastrointestinal toxicity in mice with bortezomib-resistant UMSCC-11A xenograft.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/12939461/ [2] https://pubmed.ncbi.nlm.nih.gov/17935615/ [3] https://pubmed.ncbi.nlm.nih.gov/16928830/ [4] https://pubmed.ncbi.nlm.nih.gov/21757750/ [5] https://pubmed.ncbi.nlm.nih.gov/17237265/

Aplicaciones (Applications)

Métodos	Biomarcadores	Imágenes	PMID
Western blot	p-H2AX(Ser139) / KU70 / KU80 / RAD51 / RAD52 / ERCC1 Acetyl Histone H3 / Acetyl Histone H4 / Acetyl tubulin p21 / p27 SOS1 / SOS2 PARP / p-ERK / p-p38 / p38 / p-BRAF / p-MEK / MEK		24155971
Growth inhibition assay	Cell viability IC50		24155971

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
NCT06406465	Not yet recruiting	Carcinoma Neuroendocrine\|Tumor Neuroendocrine\|Tumors Neuroendocrine\|Neuroendocrine; Carcinoma\|Small Cell; Receptors	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	May 15 2024	Phase 2
NCT04315233	Recruiting	Metastatic Breast Cancer\|Recurrent Ovarian Carcinoma	University of Utah\|Novartis\|Acrotech Biopharma	May 3 2021	Phase 1
NCT04703920	Recruiting	Metastatic Breast Cancer\|Metastatic Castration-resistant Prostate Cancer\|Metastatic Ovarian Carcinoma	University of Michigan Rogel Cancer Center\|Pfizer\|Acrotech Biopharma Inc.	March 4 2021	Phase 1
NCT03772925	Active not recruiting	Recurrent Acute Myeloid Leukemia\|Recurrent Myelodysplastic Syndrome\|Refractory Acute Myeloid Leukemia\|Refractory Myelodysplastic Syndrome	National Cancer Institute (NCI)	June 20 2019	Phase 1

Preguntas frecuentes (Frequently Asked Questions)

Pregunta 1:
Could you please give some suggestions for the use of it in vivo (i.p. injection)?

Respuesta:
For I.P. injection, it can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 10 mg/ml clearly. When preparing the solution, please dissolve this compound in DMSO clearly first. Then add PEG, after they mixed well, then dilute with water. Hope this information is useful to you.

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):