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Monastrol Kinesin inhibiteur

Name: Monastrol
Brand: Selleck Chemicals
SKU: S8439
Rating: 5 (19 reviews)

N° Cat.S8439

Monastrol ((±)-Monastrol) est un petit inhibiteur moléculaire perméable aux cellules de kinesin-5(KIF11) avec une IC50 de 14μM, qui est essentiel pour maintenir la séparation des demi-broches.

Monastrol Kinesin inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 292.35

Aller à

Contrôle qualité

Lot : Pureté : 99.86%

99.86

Cibles apparentées	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Autre Kinesin Inhibiteurs	GSK923295 Ispinesib (SB-715992) SB743921 HCl ARQ 621 K 858 BTB-1 VLS-1488(KIF18A-IN-6 ) H-Cys(Trt)-OH Filanesib hydrochloride GW406108X

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Description de lactivité	PMID
HeLa	Function assay		12 hrs	Inhibition of Eg5 ATPase activity expressed in HeLa cells after 12 hrs, IC50=6.1μM	17587586
HCT116	Cell cycle assay			Effect on cell cycle progression in human HCT116 cells assessed as mitotic arrest measured by doubling DNA content by fluorescence microscopy, EC50=1.2μM	18793847
HCT116	Cell cycle assay			Effect on cell cycle progression in human HCT116 cells assessed as increase in phospho-histone H3 by fluorescence microscopy, EC50=1.5μM	18793847
KBV1/KB3-1	Function assay			Drug resistant ratio of EC50 for human KBV1 cells overexpressing MDR1 to EC50 for KB3-1 cells, EC50=0.0012μM	20597485
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay, EC50=24.155μM	20597485
hTERT-HME1	Antiproliferative assay		72 hrs	Antiproliferative activity against human hTERT-HME1 cells after 72 hrs by Alamar blue assay, EC50=45.082μM	20597485
KBV1	Antiproliferative assay		72 hrs	Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay in presence of zosuquidar, EC50=45.394μM	20597485
HL-60(TB)	Growth inhibition assay			Growth inhibition of human HL-60(TB) cells, GI50=25.1μM	21855351
M14	Growth inhibition assay			Growth inhibition of human M14 cells, GI50=25.1μM	21855351
CCRF-CEM	Growth inhibition assay			Growth inhibition of human CCRF-CEM cells, GI50=31.6μM	21855351
K562	Growth inhibition assay			Growth inhibition of human K562 cells, GI50=31.6μM	21855351
MOLT4	Growth inhibition assay			Growth inhibition of human MOLT4 cells, GI50=31.6μM	21855351
SR	Growth inhibition assay			Growth inhibition of human SR cells, GI50=31.6μM	21855351
NCI-H522	Growth inhibition assay			Growth inhibition of human NCI-H522 cells, GI50=31.6μM	21855351
COLO205	Growth inhibition assay			Growth inhibition of human COLO205 cells, GI50=31.6μM	21855351
HCT116	Growth inhibition assay			Growth inhibition of human HCT116 cells, GI50=31.6μM	21855351
KM12	Growth inhibition assay			Growth inhibition of human KM12 cells, GI50=31.6μM	21855351
SF295	Growth inhibition assay			Growth inhibition of human SF295 cells, GI50=31.6μM	21855351
U251	Growth inhibition assay			Growth inhibition of human U251 cells, GI50=31.6μM	21855351
SK-MEL-2	Growth inhibition assay			Growth inhibition of human SK-MEL-2 cells, GI50=31.6μM	21855351
RPMI8266	Growth inhibition assay			Growth inhibition of human RPMI8266 cells, GI50=31.6μM	21855351
NCI-H322M	Growth inhibition assay			Growth inhibition of human NCI-H322M cells, GI50=39.8μM	21855351
HCC2998	Growth inhibition assay			Growth inhibition of human HCC2998 cells, GI50=39.8μM	21855351
HCT15	Growth inhibition assay			Growth inhibition of human HCT15 cells, GI50=39.8μM	21855351
SW620	Growth inhibition assay			Growth inhibition of human SW620 cells, GI50=39.8μM	21855351
SNB75	Growth inhibition assay			Growth inhibition of human SNB75 cells, GI50=39.8μM	21855351
SK-MEL-5	Growth inhibition assay			Growth inhibition of human SK-MEL-5 cells, GI50=39.8μM	21855351
UACC62	Growth inhibition assay			Growth inhibition of human UACC62 cells, GI50=39.8μM	21855351
SN12C	Growth inhibition assay			Growth inhibition of human SN12C cells, GI50=39.8μM	21855351
HL-60(TB)	Growth inhibition assay		24 hrs	Growth inhibition of human HL-60(TB) cells incubated for 24 hrs by MTT assay, IC50=0.147μM	28667871
MOLT4	Growth inhibition assay		24 hrs	Growth inhibition of human MOLT4 cells incubated for 24 hrs by MTT assay, IC50=0.215μM	28667871
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
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
McCoy	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse McCoy cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=26.8μM	29908443
MM1S	Antiproliferative assay		72 hrs	Antiproliferative activity against human MM1S cells incubated for 72 hrs by MTT assay, IC50=8.7μM	ChEMBL
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay, IC50=9μM	ChEMBL
C6	Antiproliferative assay	100 uM	24 hrs	Antiproliferative activity against rat C6 cells assessed as reduction in cell viability at 100 uM after 24 hrs by MTS assay relative to control	ChEMBL
C6	Cell cycle assay	100 uM	24 hrs	Cell cycle arrest in rat C6 cells assessed as accumulation at G2/M phase at 100 uM after 24 hrs by propidium iodide staining based flow cytometry	ChEMBL
U138MG	Apoptosis assay	200 uM	48 hrs	Induction of apoptosis in human U138MG cells at 200 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry	ChEMBL
U138MG	Necrosis assay	200 uM	48 hrs	Induction of necrosis in human U138MG cells at 200 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry	ChEMBL
C6	Apoptosis assay	100 uM	48 hrs	Induction of apoptosis in rat C6 cells at 100 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry	ChEMBL
U138MG	Function assay	200 uM	24 hrs	Inhibition of EG5 in human U138MG cells assessed as monopolar spindle formation at 200 uM after 24 hrs by Hoechst staining based immunofluorescence microscopic method	ChEMBL
C6	Function assay	100 uM	24 hrs	Inhibition of EG5 in rat C6 cells assessed as monopolar spindle formation at 100 uM after 24 hrs by Hoechst staining based immunofluorescence microscopic method	ChEMBL
C6	Antiproliferative assay	5 to 50 uM	48 hrs	Antiproliferative activity against rat C6 cells at 5 to 50 uM after 48 hrs by Neubauer chamber method	ChEMBL
MCF7	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human MCF7 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
NCI/ADR-RES	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human NCI/ADR-RES cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
786-0	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human 786-0 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
HT-29	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human HT-29 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
UACC62	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human UACC62 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
PC3	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human PC3 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
OVCAR3	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human OVCAR3 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
Cliquez pour voir plus de données expérimentales sur les lignées cellulaires

Informations chimiques, stockage et stabilité

Poids moléculaire	292.35	Formule	C₁₄H₁₆N₂O₃S	Stockage (À partir de la date de réception)	3 years -20°C(in the dark) powder
N° CAS	329689-23-8	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	(±)-Monastrol			Smiles	CCOC(=O)C1=C(NC(=S)NC1C2=CC(=CC=C2)O)C

Solubilité

In vitro
Lot:

DMSO : 58 mg/mL (198.39 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 58 mg/mL

Water : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	2.900mg/ml (9.92mM)
	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	0.710mg/ml (2.43mM)
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.

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)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

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	KIF11(Eg5) (Cell-based assay) 14 μM
In vitro	Monastrol n'inhibe pas la progression à travers les phases S et G2 du cycle cellulaire ou la duplication des centrosomes. L'arrêt mitotique dû à ce composé est également rapidement réversible. Il inhibe également la formation de fuseaux bipolaires dans les extraits d'œufs de Xénope. Ce produit chimique arrête les cellules en mitose avec des fuseaux monoastraux composés d'un réseau radial de microtubules entouré d'un anneau de chromosomes, tandis qu'il n'affecte pas les microtubules dans les cellules en interphase ou la polymérisation des microtubules in vitro. L'exposition de neurones sympathiques cultivés à ce composé pendant quelques heures augmente à la fois le nombre et le taux de croissance des axones. Avec un temps supplémentaire, les longueurs globales des axones sont indiscernables des contrôles. Les neurones sensoriels montrent une augmentation similaire à court terme du taux de croissance axonal. Cependant, une exposition prolongée entraîne des axones plus courts, suggérant que les neurones sensoriels peuvent être plus sensibles aux effets toxiques du médicament. Néanmoins, la santé globale des cultures est encore bien plus robuste que les cultures traitées au taxol, un médicament couramment utilisé pour la thérapie anticancéreuse. Dans les cellules HeLa, ce composé active le point de contrôle du fuseau, entraînant un arrêt mitotique et une apoptose.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/10973989/ [2] https://pubmed.ncbi.nlm.nih.gov/14983520/ [3] https://pubmed.ncbi.nlm.nih.gov/17041103/ [4] https://pubmed.ncbi.nlm.nih.gov/10542155/

Applications

Méthodes	Biomarqueurs	Images	PMID
Growth inhibition assay	Cell viability		26035434
Western blot	Cyclin B / Survivin		26035434

Support technique

Instructions de manipulation

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

Si vous avez dautres questions, veuillez laisser un message.

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