Home Cytoskeletal Signaling Antineoplastic and Immunosuppressive Antibiotics Inhibiteur Vinblastine sulfate

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Vinblastine sulfate Antineoplastic and Immunosuppressive Antibiotics Inhibiteur

Réf. Catalogue: S4505

Vinblastine sulfate inhibe la formation de microtubules et supprime l'activité de la nAChR avec un IC50 de 8,9 μM dans un essai acellulaire, utilisé pour traiter certains types de cancer. Ce composé induit l'Autophagy et l'apoptosis.
Vinblastine sulfate Antineoplastic and Immunosuppressive Antibiotics Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 909.05

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Contrôle Qualité (Quality Control)

Lot : Pureté : 99.91%
99.91

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires Type d'essai Concentration Temps d'incubation Formulation Description de l'activité PMID
COLO 320 human colorectal carcinoma cell line Function assay In vitro concentration required to kill 50% of COLO 320 human colorectal carcinoma cell line, EC50=0.08 μM
LNCaP human prostate cancer cell line Function assay In vitro concentration required to kill 50% of LNCaP human prostate cancer cell line, EC50=0.5 μM
K562 cell Growth inhibition assay In vitro inhibitory concentration against human chronic myelogenous leukemia K562 cell growth, IC50=0.001 μM
T47D cells Function assay In vitro concentration required to kill 50% of T47D human breast ductal carcinoma cell line, EC50=0.08 μM
K562 cell Proliferation assay 48 h Antiproliferative activity against human K562 cells after 48 hrs, IC50=0.001 μM
ACHN cells Cytotoxicity assay 48 h Cytotoxicity against human ACHN cells after 48 hrs by SRB assay, IC50=22.7 μM
A375 cells Cytotoxicity assay 48 h Cytotoxicity against human A375 cells after 48 hrs by SRB assay, IC50=7.2 μM
C32 cells Cytotoxicity assay 48 h Cytotoxicity against human C32 cells after 48 hrs by SRB assay, IC50=3 μM
LNCAP cells Cytotoxicity assay 48 h Cytotoxicity against human LNCAP cells after 48 hrs by SRB assay, IC50=29.3 μM
Huh-7D12 cells Cytotoxicity assay 48 h Cytotoxicity against human Huh-7D12 cells after 48 hrs by SRB assay, IC50=45.6 μM
COR-L23 cells Cytotoxicity assay 48 h Cytotoxicity against human COR-L23 cells after 48 hrs by SRB assay, IC50=45.5 μM
142BR cells Cytotoxicity assay 48 h Cytotoxicity against human 142BR cells after 48 hrs by SRB assay, IC50=37.6 μM
HT-29 cells Cytotoxicity assay 48 h Cytotoxicity against human HT-29 cells after 48 hrs by MTS assay, IC50=0.55 μM
A549 cells Proliferation assay 48 h Antiproliferative activity against human A549 cells after 48 hrs by MTS assay, IC50=2.36 μM
DU145 cells Proliferation assay 48 h Antiproliferative activity against human DU145 cells after 48 hrs by MTS assay, IC50=4.25 μM
SK-MEL-5 cells Proliferation assay 48 h Antiproliferative activity against human SK-MEL-5 cells after 48 hrs by MTS assay, IC50=1.74 μM
HepG2 cells Proliferation assay 48 h Antiproliferative activity against human HepG2 cells after 48 hrs by MTS assay, IC50=0.16 μM
HT-29 cells Proliferation assay 48 h Antiproliferative activity against human HT-29 cells after 48 hrs by MTS assay, IC50=11.18 μM
MCF7 cells Proliferation assay 48 h Antiproliferative activity against human MCF7 cells after 48 hrs by MTS assay, IC50=24.08 μM
MDA-MB-231 cells Proliferation assay 48 h Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTS assay, IC50=31.52 μM
rat REF52 cells Function assay 0.1 μM 30 mins Induction of microtubule depolymerization in rat REF52 cells at 0.1 uM after 30 mins by fluorescence assay
HepG2 cells Cytotoxicity assay 72 h Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.056 μM
HepG2 cells Cytotoxicity assay 72 h Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.019 μM
K562 cells Cytotoxicity assay 72 h Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.016 μM
MDA-MB-231 cells Cytotoxicity assay 72 h Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.0083 μM
MCF7 cells Cytotoxicity assay 72 h Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.007 μM
SCL6 cells Cytotoxicity assay Cytotoxicity against human SCL6 cells by MTT assay, ED50=6.1 Μm
SCL9 Cytotoxicity assay Cytotoxicity against human SCL9 cells by MTT assay, ED=5.3 μM
KATO III cells Cytotoxicity assay Cytotoxicity against human KATO III cells by MTT assay, ED50=6.1 μM
NUGC4 cells Cytotoxicity assay Cytotoxicity against human NUGC4 cells by MTT assay, ED50=5.3 μM
UACC903 cells Cytotoxicity assay 48 h Cytotoxicity against human UACC903 cells after 48 hrs by MTS assay, IC50=1.65 μM
K562 cells Function assay Inhibition of tubulin polymerization in human K562 cells, IC50=0.13 μM
BxPC3 cells Proliferation assay 48 h Antiproliferative activity against human BxPC3 cells after 48 hrs by MTS assay, IC50=1.13 μM
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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire 909.05 Formule

C46H58N4O9.H2SO4

 Stockage (À compter de la date de réception)
N° CAS 143-67-9 Télécharger le SDF Stockage des solutions mères

Synonymes NSC-49842, Vincaleukoblastine, 29060-LE Smiles CCC1(CC2CC(C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O.OS(=O)(=O)O

Solubilité (Solubility)

In vitro
Lot:

DMSO : 100 mg/mL (110.0 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : 50 mg/mL

Ethanol : 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 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

mg/kg g μL

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y 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 d'abord 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, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.

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

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (Mechanism of Action)

Targets/IC50/Ki
nAChR
(Adrenal Chromaffin Cells)
8.9 μM
In vitro
The average terminal half-lives of Vinblastine sulfate is 14.3 h. When incubated in freshly isolated rat hepatocytes, this compound penetrates rapidly and intensely into the cells, probably through a passive diffusion mechanism followed by tight cellular binding. It inhibits the angiogenic response induced by adrenomedullin and is also positive for mitotic slippage, causing micronuclei in mononucleate cells with cytokinesis block. This chemical gives significant increase in micronucleated mononucleated cells at concentrations that produced approximately 50% cell death and cytostasis or less as calculated using RPD, RICC and RCC.
In vivo
Vinblastine is a widely used anticancer drug with undesired side effects . A combination of this compound and RAP at very low doses against human HCC gets a satisfactory antiangiogenic effect in vivo. The clinically relevant dose of this chemical inhibits palmitoylation of tubulin in vivo in CEM cells (effect on depalmitoylation of tubulin).
Références
  • [4] https://pubmed.ncbi.nlm.nih.gov/14508526/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17202812/

Applications (Applications)

Méthodes Biomarqueurs Images PMID
Western blot GRP78 p-eIF2 p-JNK / c-Caspase-7 / c-PARP ERK / p-ERK / Mcl-1 / Bad / Bid / Noxa
S4505-WB1
19674193
Immunofluorescence α-tubulin / Acetyl tubulin
S4505-IF1
30120268
Growth inhibition assay Cell viability
S4505-viability1
27114800

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2026-08-20)

Numéro NCT Recrutement Conditions Promoteur/Collaborateurs Date de début Phases
NCT06745076 RECRUITING
Advanced Hodgkin Lymphoma; Classic Hodgkin Lymphoma; Lugano Classification Stage III Hodgkin Lymphoma AJCC v8; Lugano Classification Stage IV Hodgkin Lymphoma AJCC v8
University of Washington
 2025-03-06 PHASE2
NCT05180825 RECRUITING
Grade 1 Glioma; Mixed Glio-neuronal Tumors; Pleomorphic Xanthoastrocytoma
University Hospital, Strasbourg, France
 2022-05-05 PHASE2
NCT05675410 RECRUITING
Lugano Classification Limited Stage Hodgkin Lymphoma AJCC v8
National Cancer Institute (NCI)
 2023-05-11 PHASE3
NCT07551583 RECRUITING
Hodgkin Lymphoma
M.D. Anderson Cancer Center
 2026-08-19 PHASE2
NCT04685616 RECRUITING
Hodgkin Lymphoma
University College, London
 2022-04-14 PHASE3
NCT06666348 RECRUITING
Pediatric Low-grade Glioma
St. Justine's Hospital
 2026-01-12 PHASE1; PHASE2