Home Cytoskeletal Signaling Microtubule Associated inhibiteur Combretastatin A4

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Combretastatin A4 Microtubule Associated inhibiteur

N° Cat.S7783

Combretastatin A4 est un agent ciblant les microtubules qui se lie à la β-tubuline avec un Kd de 0,4 μM. Phase 3.
Combretastatin A4 Microtubule Associated inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 316.35

Aller à

Contrôle qualité

Lot : S778301 DMSO]63 mg/mL]false]Ethanol]34 mg/mL]false]Water]Insoluble]false Pureté : 99.87%
99.87

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires Type dessai Concentration Temps dincubation Formulation Description de lactivité 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
Cliquez pour voir plus de données expérimentales sur les lignées cellulaires

Informations chimiques, stockage et stabilité

Poids moléculaire 316.35 Formule

C18H20O5

 Stockage (À partir de la date de réception)
N° CAS 117048-59-6 Télécharger le SDF Stockage des solutions mères

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

Solubilité

In vitro
Lot:

DMSO : 63 mg/mL (199.14 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 34 mg/mL

Water : Insoluble

Calculateur de molarité

Masse Concentration Volume Poids moléculaire
Calculateur de dilution Calculateur de poids moléculaire

In vivo
Lot:

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

mg/kg g μL

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH2O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC50/Ki
β-tubulin
0.4 μM(Kd)
In vitro
Combretastatin A4 inhibe la croissance des cellules MDA-MB-231, A549, Hela, HL-60, SF295, HCT-8, MDA-MB435, PC3M, OVCAR-8, NCI-H358M et des lymphocytes avec un IC50 de 2,8, 3,8, 0,9, 2,1, 6,2, 5,3, 7,9, 4,7, 0,37, 8 et 3,2 nM, respectivement. 1 μM de ce composé inhibe la polymérisation de la tubuline de 35%, et 10 μM bloque presque complètement la polymérisation de la tubuline. Ce produit chimique démontre une grande capacité de liaison relative, atteignant 78% de la liaison de la colchicine.
Kinase Assay
Essai de liaison compétitive utilisant LC-MS/MS
La colchicine (1,2 μM) est incubée avec de la tubuline (1,3 mg/mL) dans le tampon d'incubation (80 mM PIPES, 2,0 mM MgCl2, 0,5 mM EGTA, pH 6,9) à 37℃ pendant 1 h. Des concentrations variables (0,1 − 125 μM) de ce composé sont utilisées pour concurrencer la colchicine initialement liée à la tubuline. Après incubation, le filtrat est obtenu. La capacité de l'analogue à inhiber la liaison de la colchicine est exprimée en pourcentage de la liaison de contrôle en l'absence de tout compétiteur.
In vivo
Dans le modèle de tumeur mammaire NT2 et MDA-MB-231, l'administration de Combretastatin A4 (100 mg/kg, i.p.) induit une diminution significative des lipides R1 et une réduction du pO2 tumoral mesuré par oximétrie par résonance paramagnétique électronique (RPE). Ce composé (100 mg/kg, i.p.) diminue significativement la Ktrans chez les souris NMRI mâles.
Références

Support technique

Instructions de manipulation

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Questions fréquemment posées

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

Réponse :
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.