Vinblastine sulfate Antineoplastic and Immunosuppressive Antibiotics Inibitore

N. Cat.: S4505

Vinblastine sulfate inibisce la formazione dei microtubuli e sopprime l'attività di nAChR con un IC50 di 8,9 μM in un saggio senza cellule, utilizzato per trattare alcuni tipi di cancro. Questo composto induce autophagy e apoptosis.
Vinblastine sulfate Antineoplastic and Immunosuppressive Antibiotics Inibitore Chemical Structure

Struttura chimica

Peso molecolare: 909.05

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.91%
99.91

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dell'attività 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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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 909.05 Formula

C46H58N4O9.H2SO4

Conservazione (Dalla data di ricezione)
N. CAS 143-67-9 Scarica SDF Conservazione delle soluzioni stock

Sinonimi 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

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 100 mg/mL (110.0 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : 50 mg/mL

Ethanol : Insoluble

Calcolatore di Molarità

Massa Concentrazione Volume Peso molecolare
Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo
Lotto:

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (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).
Riferimenti
  • [4] https://pubmed.ncbi.nlm.nih.gov/14508526/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17202812/

Applicazioni (Applications)

Metodi Biomarcatori Immagini 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

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2026-08-20)

Numero NCT Reclutamento Condizioni Sponsor/Collaboratori Data di inizio Fasi
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