Home Cytoskeletal Signaling Microtubule Associated inhibidor Combretastatin A4

solo para uso en investigación

Combretastatin A4 Microtubule Associated inhibidor

Cat. No.S7783

Combretastatin A4 es un agente dirigido a microtubules que se une a la β-tubulina con un Kd de 0,4 μM. Fase 3.
Combretastatin A4 Microtubule Associated inhibidor Chemical Structure

Estructura química

Peso molecular: 316.35

Saltar a

Control de calidad

Lote: S778301 DMSO]63 mg/mL]false]Ethanol]34 mg/mL]false]Water]Insoluble]false Pureza: 99.87%
99.87

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad PMID
SKMEL-5 Growth inhibition assay Cytotoxic concentration required to inhibit 50% cell growth in SKMEL-5 melanoma cell lines, ED50=3.00E-08 μM
A-549 Growth inhibition assay Cytotoxic concentration required to inhibit 50% cell growth in A-549 lung carcinoma cell lines, ED50=1.20E-06 μM
MCF-7 Growth inhibition assay Cytotoxic concentration required to inhibit 50% cell growth in MCF-7 breast carcinoma cell lines, ED50=3.80E-06 μM
HT-29 Growth inhibition assay Cytotoxic concentration required to inhibit 50% cell growth in HT-29 colon adenocarcinoma cell lines, ED50=1.20E-06 μM
MLM melanoma cell Growth inhibition assay Cytotoxic concentration required to inhibit 50% cell growth in MLM melanoma cell lines, ED50=1.40E-06 μM
M14 Cytotoxicity assay In vitro cytotoxic activity was tested against human melanoma cancer (M14) cell line, GI50=0.0001 μM
SK-OV3 Cytotoxicity assay In vitro cytotoxic activity tested against human ovarian cancer (SK-OV3) cell line, GI50=0.0001 μM
HL60 cells Cytotoxicity assay 72 h Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.0001 μM
SK-OV-3 Growth inhibition assay 48 h Growth inhibition of human SK-OV-3 after 48 hrs by SRB assay, GI50=0.00013 μM
HepG2 cells Cytotoxicity assay Cytotoxicity against human HepG2 cells, IC50=0.00014 μM
ZR-75-1 Cytotoxicity assay Cytotoxicity against ZR-75-1 cell line, IC50=0.00024 μM
HeLa cell Cytotoxicity assay Cytotoxicity against HeLa cell line, IC50=0.0003 μM
HCT116 cell Cytotoxicity assay Cytotoxicity against HCT116 cell line, IC50=0.00035 μM
KBV1 cells Cytotoxicity assay 72 h Cytotoxicity against human vinblastine-resistant KBV1 cells after 72 hrs by MTT assay, IC50=0.0004 μM
SKOV3 Cytotoxicity assay Cytotoxicity against human SKOV3 cells by SRB assay, GI50=0.00042 μM
SKOV3 cells Growth inhibition assay Growth inhibition of human SKOV3 cells by sulforhodamine B assay, GI50=0.00042 μM
HeLa cells Cytotoxicity assay Cytotoxicity against human HeLa cells by MTT assay, IC50=0.00051 μM
DU145 cells Cytotoxicity assay Cytotoxicity against human DU145 cells by SRB assay, GI50=0.00054 μM
DU145 cells Growth inhibition assay Growth inhibition of human DU145 cells by sulforhodamine B assay, GI50=0.00054 μM
SK-N-BE Proliferation assay 72 h Antiproliferative activity in human SK-N-BE cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00058 μM
NCIH460 cells Cytotoxicity assay 48 h Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay, GI50=0.0006 μM
KB-VIN10 cells Proliferation assay 72 h Antiproliferative activity against human KB-VIN10 cells over-expressing P-gp 170/MDR1 after 72 hrs by methylene blue assay, IC50=0.0007 μM
HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against human HCT116 cells assessed as reduction of [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50=0.00074 μM
DU145 cells Cytotoxicity assay 48 h Cytotoxicity against human DU145 cells after 48 hrs by SRB assay, GI50=0.0008 μM
RS4:11 cells Proliferation assay 72 h Antiproliferative activity against human RS4:11 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test, IC50=0.0008 μM
HCT 116 Growth inhibition assay Concentration which produces 50% inhibition of growth of human colon tumor HCT 116, IC50=0.0009 μM
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by resazurin based fluorescence assay, IC50=0.0009 μM
BNL 1ME A.7R.1 cells Cytotoxicity assay Cytotoxicity against mouse BNL 1ME A.7R.1 cells, IC50=0.0009 μM
Calu6 Proliferation assay 48 h Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry, IC50=0.00094 μM
melanoma B16 cell Growth inhibition assay Concentration which produces 50% inhibition of growth of murine melanoma B16 cell line, IC50=0.001 μM
DU145 cells Cytotoxicity assay Cytotoxicity against human DU145 cells by SRB assay, GI50=0.001 μM
HCT116 cells Proliferation assay 72 h Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50=0.001 μM
HCT15 cells Proliferation assay 72 h Antiproliferative activity against human HCT15 cells after 72 hrs by MTS assay, IC50=0.001 μM
HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.001 μM
A10 cells Growth inhibition assay 48 h Growth inhibition of rat A10 cells after 48 hrs by MTT assay, IC50=0.001 μM
HUVEC cells Growth inhibition assay 48 h Growth inhibition of HUVEC cells after 48 hrs by MTT assay, IC50=0.001 μM
HL60 cells Cytotoxicity assay 72 h Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.001 μM
NCI-H522 cells Growth inhibition assay 48 h Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay, GI50=0.001 μM
MDA-MB-435 cells Growth inhibition assay 48 h Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay, GI50=0.001 μM
OVCAR3 Growth inhibition assay 48 h Growth inhibition of human OVCAR3 cells after 48 hrs by SRB assay, GI50=0.001 μM
NCI/ADR-RES cells Growth inhibition assay 48 h Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay, GI50=0.001 μM
PC3 cells Growth inhibition assay 48 h Growth inhibition of human PC3 cells after 48 hrs by SRB assay, GI50=0.001 μM
DU145 cells Growth inhibition assay 48 h Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.001 μM
MDA-MB-231 cells Growth inhibition assay 48 h Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay, GI50=0.001 μM
CEM cells Cytotoxicity assay 72 h Cytotoxicity against human CEM cells after 72 hrs by MTT assay, IC50=0.001 μM
HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.001 μM
MDA-MB-435 cells Cytotoxicity assay 72 h Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50=0.001 μM
HaCaT cells Proliferation assay Antiproliferative activity against human HaCaT cells assessed as cell viability by MTT assay, IC50=0.001 μM
HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test, IC50=0.001 μM
HT-29 Growth inhibition assay Growth inhibition of human HT-29 cells by MTT assay, IC50=0.001 μM
HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
Hs578T cells Growth inhibition assay 48 h Growth inhibition of human Hs578T cells after 48 hrs by SRB assay, GI50=0.001 μM
HL60 cells Cytotoxicity assay 72 h Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
SKOV3 cells Growth inhibition assay Growth inhibition of human SKOV3 cells by MTT assay, IC50=0.001 μM
MDA-MB-468 cells Cytotoxicity assay 4 days Cytotoxicity against human MDA-MB-468 cells assessed as cell viability after 4 days by MTS assay, IC50=0.0011 μM
MCF7 cells Proliferation assay 72 h Antiproliferative activity in human MCF7 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00111 μM
H460 Cytotoxicity assay Cytotoxicity against human H460 cells by sulforhodamine B test, IC50=0.0012 μM
H460 Proliferation assay Antiproliferative activity against human H460 cells, IC50=0.00124 μM
NCI-H460 cells Cytotoxicity assay 72 h Cytotoxic activity against human NCI-H460 cells after 72 hrs by sulforhodamine B test, IC50=0.0013 μM
OVCAR8 cells Growth inhibition assay 96 h Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs, IC50=0.0013 μM
NCI/ADR-RES cells Cytotoxicity assay Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM
OVCAR8 cells Cytotoxicity assay 96 h Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy, IC50=0.0013 μM
NCI/ADR-RES cells Cytotoxicity assay 96 h Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy, IC50=0.0013 μM
OVCAR8 cells Cytotoxicity assay Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM
HuTu 80 cells Proliferation assay 72 h Antiproliferative activity in human HuTu 80 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00137 μM
K562 cells Cytotoxicity assay Cytotoxicity against human K562 cells, IC50=0.0014 μM
NCI/ADR (MDR) cells Function assay Cell cycle arrest in NCI/ADR (MDR) cells by accumulation at G2/M phase, IC50=0.0015 μM
HUVEC Proliferation assay Antiproliferative activity against human HUVEC, IC50=0.0015 μM
KB cell Proliferation assay Antiproliferative activity against human KB cell line by methylene blue dye assay, IC50=0.0015 μM
KB-VIN10 cell Proliferation assay Antiproliferative activity against human KB-VIN10 cell line by methylene blue dye assay, IC50=0.0015 μM
Human SH-SY5Y neuroblastoma cells Function assay Inhibitory concentration against Human SH-SY5Y neuroblastoma cells, IC50=0.0015 μM
SW620 cells Proliferation assay 72 h Antiproliferative activity in human SW620 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00152 μM
Molt4/C8 cells Proliferation assay Antiproliferative activity against human Molt4/C8 cells, IC50=0.0016 μM
ACHN cell Proliferation assay Antiproliferative activity against drug resistant ACHN cell line expressing MDR1 by Alamar Blue assay, IC50=0.0016 μM
Molt4/C8 cells Proliferation assay 3 days Antiproliferative effect against human Molt4/C8 cells after 3 days, IC50=0.0016 μM
Haga clic para ver más datos experimentales de líneas celulares

Información química, almacenamiento y estabilidad

Peso molecular 316.35 Fórmula

C18H20O5

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 117048-59-6 Descargar SDF Almacenamiento de soluciones madre

Sinónimos N/A Smiles COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)O

Solubilidad

In vitro
Lote:

DMSO : 63 mg/mL (199.14 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 34 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

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)

mg/kg g μL

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
β-tubulin
0.4 μM(Kd)
In vitro
Combretastatin A4 inhibe el crecimiento de células MDA-MB-231, A549, Hela, HL-60, SF295, HCT-8, MDA-MB435, PC3M, OVCAR-8, NCI-H358M y linfocitos con una IC50 de 2,8, 3,8, 0,9, 2,1, 6,2, 5,3, 7,9, 4,7, 0,37, 8 y 3,2 nM, respectivamente. 1 μM de este compuesto inhibe la polimerización de tubulina en un 35 %, y 10 μM bloquean casi completamente la polimerización de tubulina. Este producto químico demuestra una gran capacidad de unión relativa, alcanzando el 78 % de la unión a colchicina.
Ensayo de quinasa
Ensayo de unión competitiva usando LC-MS/MS
La colchicina (1,2 μM) se incuba con tubulina (1,3 mg/mL) en el tampón de incubación (80 mM PIPES, 2,0 mM MgCl2, 0,5 mM EGTA, pH 6,9) a 37 ℃ durante 1 h. Se utilizan concentraciones variables (0,1 − 125 μM) de este compuesto para competir con la colchicina unida originalmente a la tubulina. Después de la incubación, se obtiene el filtrado. La capacidad del análogo para inhibir la unión de la colchicina se expresa como un porcentaje de la unión de control en ausencia de cualquier competidor.
In vivo
En el modelo de tumor mamario NT2 y MDA-MB-231, la administración de Combretastatin A4 (100 mg/kg, i.p.) induce una disminución significativa de los lípidos R1 y una reducción de la pO2 tumoral medida por oximetría de resonancia paramagnética electrónica (EPR). Este compuesto (100 mg/kg, i.p.) disminuye significativamente la Ktrans en ratones NMRI machos.
Referencias

Soporte técnico

Instrucciones de manipulación

Tel: +1-832-582-8158 Ext:3

Si tiene alguna otra consulta, por favor deje un mensaje.

Por favor, introduzca su nombre.
Por favor, introduzca su correo electrónico. Por favor, introduzca una dirección de correo electrónico válida.
Por favor, escríbanos algo.

Preguntas frecuentes

Pregunta 1:
How to make solution for in vivo IP injection of it?

Respuesta:
We've tested some vehicles for this compound, and found it can be dissolved in 5% DMSO+50% PEG 300+ddH2O at 30mg/ml clearly. When prepare the solution, please dissolve it in DMSO clearly first. Then add PEG, after they mixed well, then dilute with water.