product name Vinblastine
Description: Vinblastine (also known as NSC49842), a natural alkaloid isolated from the plant Vinca rosea Linn, is a mitotic inhibitor that inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, it is used to treat certain kinds of cancer. Vinblastine binds to tubulin and inhibits microtubule formation, resulting in disruption of mitotic spindle assembly and arrest of tumor cells in the M phase of the cell cycle.
References: Proc Soc Exp Biol Med. 1993 Jul;203(3):372-6; Oncogene. 2003 Sep 25;22(41):6458-61.
909.05
Formula
C46H58N4O9.H2SO4
CAS No.
143-67-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (110.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
NSC49842
other peoduct :
| In Vitro |
In vitro activity: The average terminal half-lives of Vinblastine is 14.3 h. When incubated in freshly isolated rat hepatocytes, VLB penetrates rapidly and intensely into the cells, probably through a passive diffusion mechanism followed by tight cellular binding. Vinblastine inhibits the angiogenic response induced by adrenomedullin and is also positive for mitotic slippage, causing micronuclei in mononucleate cells with cytokinesis block. vinblastine 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. Kinase Assay: Cell Assay: Six-well treatment plates are set up that contained 5 × 104 cells/mL (Chinese hamster ovary (CHO) cells) in each well, suspended in 3 mL culture medium, and these are treated with vinblastine for 3 h followed by 21 h growth. |
|---|---|
| In Vivo | Vinblastine is a widely used anticancer drug with undesired side effects. A combination of VBL and RAP at very low doses against human HCC gets a satisfactory antiangiogenic effect in vivo. The clinically relevant dose of vinblastine inhibits palmitoylation of tubulin in vivo in CEM cells (effect on depalmitoylation of tubulin). |
| Animal model | |
| Formulation & Dosage | |
| References | Proc Soc Exp Biol Med. 1993 Jul;203(3):372-6; Oncogene. 2003 Sep 25;22(41):6458-61. |
