Vinblastine sulfate  (Synonyms: Vincaleukoblastine sulfate salt)

Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC₅₀ of 8.9 μM.

IC50: 8.9 μM(nAChR)^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

909.05

C₄₆H₆₀N₄O₁₃S

143-67-9

Solid

White to off-white

[H][C@@]12C[C@@](C3=C(OC)C=C(N([C@]4([H])[C@@]56[C@]7([H])[C@](C=CCN7CC6)(CC)[C@@H](OC(C)=O)[C@@]4(C(OC)=O)O)C)C5=C3)(C(OC)=O)C(NC8=C9C=CC=C8)=C9CC[N@](C2)C[C@](O)(CC)C1.OS(=O)(O)=O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. McKay DB, et al. Nicotinic and nonnicotinic receptor-mediated actions of vinblastine. Proc Soc Exp Biol Med. 1993 Jul;203(3):372-6.  [Content Brief]

  [2]. Pandya P, et al. Molecular recognition pattern of cytotoxic alkaloid vinblastine with multiple targets. J Mol Graph Model. 2014 Nov;54:1-9.  [Content Brief]

  [3]. Calvi?o 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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]