Vinblastine

SKU: orb1685623

Description

Vinblastine is a microtubule-disrupting agent that also inhibits nicotinic acetylcholine receptor (nAChR) activity with an IC50 of 8.9 µM. It is widely used in cancer research, particularly for studying mitotic arrest and apoptosis in both in vitro cell cultures and in vivo tumor models.

Research Area

Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 865-21-4
• MW: 810.97
• Purity: 97.42% (May vary between batches)
• Formula: C₄₆H₅₈N₄O₉
• SMILES: [H][C@@]12N3CC[C@@]11c4cc(c(OC)cc4N(C)[C@@]1([H])[C@](O)([C@H](OC(C)=O)[C@]2(CC)C=CC3)C(=O)OC)[C@]1(C[C@@]2([H])CN(C[C@](O)(CC)C2)CCc2c1[nH]c1ccccc21)C(=O)OC
• Target: Microtubule Associated,AChR
• Solubility: DMSO:42 mg/mL (51.79 mM);Ethanol:6 mg/mL (7.4 mM)

Bioactivity

• Target IC50:
  nAChR:8.9 μM
• 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.
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• 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. 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. 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Vinblastine, nAChR, Microtubule Associated, MicrotubuleAssociated

Compound Identifiers

PubChem CID

13342