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Vinblastine

Catalog No. T6721   CAS 865-21-4

Vinblastine inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM, used to treat certain kinds of cancer.

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Vinblastine Chemical Structure
Vinblastine, CAS 865-21-4
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Vinblastine inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM, used to treat certain kinds of cancer.
Targets&IC50 nAChR:8.9 μM
In vitro Vinblastine does not depolymerize spindle microtubules, yet it powerfully blocks mitosis (for example, IC50 0.8 nM in HeLa cells) and cells die by apoptosis[2]. In NB4 cells, vinblastine produces alteration of p53 and DNA fragmentation. Vinblastine treatment has an antiproliferative effect via the induction of apoptosis producing Bax/Bcl-2 imbalance. Vinblastine treatment suppresses NFκB expression and depresses NFκB-DNA binding activity while maintaining JNK activation that subsequently results in apoptotic response through caspase-dependent pathway[3]. Vinblastine is found to trigger apoptosis as evidenced by the loss of mitochondrial membrane potential, the release of both cytochrome c and apoptosis inducing factor, activation of caspase-9 and 3, and cleavage of Poly (ADP-ribose)-Polymerase[4].
In vivo Vinblastine is a widely used anticancer drug with undesired side effects. Its conjugation with carrier molecules could be an efficient strategy to reduce these side effects[5].
Cell Research Six-well treatment plates are set up that contained 5 × 104 cells/mL in each well, suspended in 3 mL culture medium, and these are treated with vinblastine for 3 h followed by 21 h growth. (Only for Reference)
Molecular Weight 810.97
Formula C46H58N4O9
CAS No. 865-21-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 6 mg/mL (7.39 mM)

DMSO: 42 mg/mL

TargetMolReferences and Literature

1. McKay DB, et al. Nicotinic and nonnicotinic receptor-mediated actions of vinblastine. Proc Soc Exp Biol Med. 1993 Jul;203(3):372-6. 2. Pandya P, et al. Molecular recognition pattern of cytotoxic alkaloid vinblastine with multiple targets. J Mol Graph Model. 2014 Nov;54:1-9. 3. Calviño E, et al. JNK and NFκB dependence of apoptosis induced by vinblastine in human acute promyelocytic leukaemia cells. Cell Biochem Funct. 2015 Jun;33(4):211-9. 4. Selimovic D, et al. Vinblastine-induced apoptosis of melanoma cells is mediated by Ras homologous A protein (Rho A) via mitochondrial and non-mitochondrial-dependent mechanisms. Apoptosis. 2013 Aug;18(8):980-97. 5. Bánóczi Z, et al. Synthesis and in vitro antitumor effect of vinblastine derivative-oligoarginine conjugates. Bioconjug Chem. 2010 Nov 17;21(11):1948-55.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library

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Keywords

Vinblastine 865-21-4 Cytoskeletal Signaling Neuroscience AChR Microtubule Associated inhibitor inhibit

 

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