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AZD6482 PI3K inhibidor

Name: AZD6482
Brand: Selleck Chemicals
SKU: S1462
Rating: 5 (27 reviews)

Cat. No.S1462

AZD6482 (KIN-193) es un inhibidor de PI3Kβ con un IC50 de 10 nM, 8, 87 y 109 veces más selectivo para PI3Kβ que para PI3Kδ, PI3Kα y PI3Kγ en ensayos sin células. Fase 1.

AZD6482 PI3K inhibidor Chemical Structure

Estructura química

Peso molecular: 408.45

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Control de calidad

Lote: Pureza: 99.92%

99.92

Dianas relacionadas	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Otros PI3K Inhibidores	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) LY294002 XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549)

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Descripción de la actividad
human RXF393 cell	Growth inhibition assay	Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.01154 μM
human SW982 cell	Growth inhibition assay	Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.03584 μM
human MAD-MB-468 cells	Function assay	Inhibition of PI3Kbeta in human MAD-MB-468 cells assessed as inhibition of Ser473 Akt phosphorylation by cellular potency assay, IC50=0.04 μM
human KURAMOCHI cell	Growth inhibition assay	Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=0.1051 μM
human A498 cell	Growth inhibition assay	Inhibition of human A498 cell growth in a cell viability assay, IC50=0.11795 μM
human YT cell	Growth inhibition assay	Inhibition of human YT cell growth in a cell viability assay, IC50=0.12066 μM
human VMRC-RCZ cell	Growth inhibition assay	Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=0.14898 μM
human MDA-MB-415 cell	Growth inhibition assay	Inhibition of human MDA-MB-415 cell growth in a cell viability assay, IC50=0.16732 μM
human J82 cell	Growth inhibition assay	Inhibition of human J82 cell growth in a cell viability assay, IC50=0.47779 μM
human SW1710 cell	Growth inhibition assay	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=0.5292 μM
human T47D cell	Growth inhibition assay	Inhibition of human T47D cell growth in a cell viability assay, IC50=0.5327 μM
human SU-DHL-1 cell	Growth inhibition assay	Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=0.56813 μM
human BT-20 cell	Growth inhibition assay	Inhibition of human BT-20 cell growth in a cell viability assay, IC50=0.59222 μM
human OS-RC-2 cell	Growth inhibition assay	Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=0.62388 μM
human RPMI-6666 cell	Growth inhibition assay	Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=0.64379 μM
human OVCAR-3 cell	Growth inhibition assay	Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=0.67946 μM
human NALM-6 cell	Growth inhibition assay	Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=0.70465 μM
human RS4-11 cell	Growth inhibition assay	Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=0.73806 μM
human SK-MES-1 cell	Growth inhibition assay	Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50=0.78967 μM
human ES7 cell	Growth inhibition assay	Inhibition of human ES7 cell growth in a cell viability assay, IC50=0.81286 μM
human NCI-H2342 cell	Growth inhibition assay	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=0.84294 μM
human SCC-9 cell	Growth inhibition assay	Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=0.8577 μM
human EW-7 cell	Growth inhibition assay	Inhibition of human EW-7 cell growth in a cell viability assay, IC50=0.86356 μM
human HH cell	Growth inhibition assay	Inhibition of human HH cell growth in a cell viability assay, IC50=0.96222 μM
human A427 cell	Growth inhibition assay	Inhibition of human A427 cell growth in a cell viability assay, IC50=0.99505 μM
human Daudi cell	Growth inhibition assay	Inhibition of human Daudi cell growth in a cell viability assay, IC50=1.06888 μM
human P30-OHK cell	Growth inhibition assay	Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=1.07138 μM
human HGC-27 cell	Growth inhibition assay	Inhibition of human HGC-27 cell growth in a cell viability assay， IC50=1.1816 μM
human CAMA-1 cell	Growth inhibition assay	Inhibition of human CAMA-1 cell growth in a cell viability assay, IC50=1.2001 μM
human SK-OV-3 cell	Growth inhibition assay	Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=1.20444 μM
human NCI-H1048 cell	Growth inhibition assay	Inhibition of human NCI-H1048 cell growth in a cell viability assay, IC50=1.22579 μM
human MEL-HO cell	Growth inhibition assay	Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=1.24238 μM
human NKM-1 cell	Growth inhibition assay	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.28636 μM
human NCI-H650 cel	Growth inhibition assay	Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=1.30076 μM
human HAL-01 cell	Growth inhibition assay	Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=1.30175 μM
human 786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.31283 μM
human GI-1 cell	Growth inhibition assay	Inhibition of human GI-1 cell growth in a cell viability assay, IC50=1.31808 μM
human Becker cell	Growth inhibition assay	Inhibition of human Becker cell growth in a cell viability assay, IC50=1.36315 μM
human CCF-STTG1 cell	Growth inhibition assay	Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=1.42525 μM
human MC116 cell	Growth inhibition assay	Inhibition of human MC116 cell growth in a cell viability assay, IC50=1.46122 μM
human MDA-MB-468 cell	Growth inhibition assay	Inhibition of human MDA-MB-468 cell growth in a cell viability assay, IC50=1.53736 μM
human NB12 cell	Growth inhibition assay	Inhibition of human NB12 cell growth in a cell viability assay, IC50=1.54842 μM
human LXF-289 cell	Growth inhibition assay	Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.55104 μM
human MFE-296 cell	Growth inhibition assay	Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=1.56836 μM
human SNU-423 cell	Growth inhibition assay	Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=1.57192 μM
human NCI-H2291 cell	Growth inhibition assay	Inhibition of human NCI-H2291 cell growth in a cell viability assay, IC50=1.5761 μM
human OCUB-M cell	Growth inhibition assay	Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=1.58314 μM
human KU812 cell	Growth inhibition assay	Inhibition of human KU812 cell growth in a cell viability assay, IC50=1.59628 μM
human HuO9 cell	Growth inhibition assay	Inhibition of human HuO9 cell growth in a cell viability assay, IC50=1.6128 μM
human 639-V cell	Growth inhibition assay	Inhibition of human 639-V cell growth in a cell viability assay, IC50=1.63144 μM
human HCC70 cell	Growth inhibition assay	Inhibition of human HCC70 cell growth in a cell viability assay, IC50=1.66146 μM
human SNB75 cell	Growth inhibition assay	Inhibition of human SNB75 cell growth in a cell viability assay, IC50=1.66508 μM
human D-336MG cell	Growth inhibition assay	Inhibition of human D-336MG cell growth in a cell viability assay, IC50=1.6688 μM
human LoVo cell	Growth inhibition assay	Inhibition of human LoVo cell growth in a cell viability assay, IC50=1.73825 μM
human EB2 cell	Growth inhibition assay	Inhibition of human EB2 cell growth in a cell viability assay, IC50=1.75019 μM
human HSC-2 cell	Growth inhibition assay	Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=1.75727 μM
human D-542MG cell	Growth inhibition assay	Inhibition of human D-542MG cell growth in a cell viability assay, IC50=1.85077 μM
human COLO-684 cell	Growth inhibition assay	Inhibition of human COLO-684 cell growth in a cell viability assay, IC50=2.20032 μM
human GDM-1 cell	Growth inhibition assay	Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=2.24206 μM
human SW1088 cell	Growth inhibition assay	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.48143 μM
human SF295 cell	Growth inhibition assay	Inhibition of human SF295 cell growth in a cell viability assay, IC50=2.76955 μM
human NCI-H2030 cell	Growth inhibition assay	Inhibition of human NCI-H2030 cell growth in a cell viability assay, IC50=2.90288 μM
human NCI-H1755 cell	Growth inhibition assay	Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=3.27063 μM
human MDA-MB-361 cell	Growth inhibition assay	Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=3.52709 μM
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Información química, almacenamiento y estabilidad

Peso molecular	408.45	Fórmula	C₂₂H₂₄N₄O₄	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	1173900-33-8	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	KIN-193			Smiles	CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3C(=O)O)N4CCOCC4

Solubilidad

In vitro
Lote:

DMSO : 82 mg/mL (200.75 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 10 mg/mL

Water : 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.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	30.000mg/ml (73.45mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.

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

Targets/IC₅₀/Ki	PI3Kβ (Cell-free assay) 10 nM PI3Kδ (Cell-free assay) 80 nM DNA-PK (Cell-free assay) 420 nM PI3Kα (Cell-free assay) 870 nM
In vitro	AZD6482 también inhibe PI3Kα, γ y δ, con un IC50 de 80 nM a 1,09 μM, que son significativamente más bajos que su (+)-enantiómero (forma S). Este compuesto es un agente antiplaquetario; bloquea la activación/agregación plaquetaria y promueve la desagregación plaquetaria en el ensayo de agregación plaquetaria lavada (WPA), con un valor de IC50 de 6 nM. Además, al dirigirse a PI3Kβ, este químico inhibe específicamente la trombosis sin interferir con la hemostasia normal. Por lo tanto, se utiliza como un fármaco antitrombótico para la profilaxis de trastornos trombóticos.
Ensayo de quinasa	Ensayo de inhibición enzimática de PI3K
Ensayo de quinasa	La inhibición de PI3Kβ, PI3Kα, PI3Kγ y PI3Kδ se evalúa en un ensayo de actividad enzimática basado en AlphaScreen utilizando enzimas recombinantes humanas. El ensayo mide la conversión de PIP2 a PIP3 mediada por PI3K. El PIP3 biotinilado, un dominio de homología de pleckstrina (PH) marcado con GST y las dos perlas AlphaScreen forman un complejo que emite una señal tras la excitación con láser a 680 nm. El PIP3 formado en la reacción enzimática compite con el PIP3 biotinilado por la unión al dominio PH, reduciendo así la señal con el aumento del producto enzimático. Este compuesto se disuelve en DMSO y se añade a placas de 384 pocillos. PBKβ, PBKα, PBKγ o PBKδ se añade en un tampón Tris (50 mM Tris pH 7,6, 0,05 % CHAPS, 5 mM DTT y 24 mM MgCl₂) y se deja preincubar con este producto químico durante 20 minutos antes de la adición de la solución de sustrato que contiene PIP2 y ATP. La reacción enzimática se detiene después de 20 minutos mediante la adición de una solución de parada que contiene EDTA y biotina-PIP3, seguida de la adición de una solución de detección que contiene GST-grpl PH y perlas AlphaScreen. Las placas se dejan durante un mínimo de 5 horas en la oscuridad antes del análisis. La concentración final de DMSO, ATP y PIP2 en el ensayo son, respectivamente, 0,8 %, 4 μM y 40 μM. Los valores de IC50 se calculan según la ecuación, y = {a+[(b-a)/(l+(x/IC50)^s)]}, donde y = % de inhibición; a = 0 %; b = 100 %; s = la pendiente de la curva de concentración-respuesta; x = la concentración de este compuesto.
Referencias	[1] http://www.wipo.int/patentscope/search/en/WO2009093972

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