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Vincristine sulfate(Leurocristine)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vincristine sulfate(Leurocristine)图片
CAS NO:2068-78-2
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)923.04
FormulaC46H58N4O14S
CAS No.2068-78-2 (sulfate);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (108.3 mM)
Water: 60 mg/mL (65.0 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)Saline: 30 mg/mL
Synonyms

Leurocristine; NSC-67574 sulfate; 22-Oxovincaleukoblastine sulfate; leurocristine sulfate; NSC67574; NSC 67574; Vincasar PFS, Oncovin, VCR

Chemical Name: (3aR,3a1R,4R,5S,5aR,10bR)-methyl 4-acetoxy-3a-ethyl-9-((3S,5S,7S,9S)-5-ethyl-5-hydroxy-9-(methoxycarbonyl)-2,4,5,6,7,8,9,10-octahydro-1H-3,7-methano[1]azacycloundecino[5,4-b]indol-9-yl)-6-formyl-5-hydroxy-8-methoxy-3a,3a1,4,5,5a,6,11,12-octahydro-1H-indolizino[8,1-cd]carbazole-5-carboxylate sulfate.

SMILES Code: O=C([C@]1(O)[C@]2([H])N(C=O)C3=C(C=C([C@@]4(C(OC)=O)C[C@@]5([H])C[C@@](O)(CC)C[N@](C5)CCC6=C4NC7=C6C=CC=C7)C(OC)=C3)[C@]2(CCN8CC=C9)[C@]8([H])[C@]9(CC)[C@H]1OC(C)=O)OC.O=S(O)(O)=O

实验参考方法
In Vitro

In vitro activity: Vincristine inhibits net addition of tubulin dimers at assembly ends of steady-state microtubules with Ki of 85 NM. At low concentrations, Vincristine stabilizes the spindle apparatus resulting in failure of the chromosomes to segregate leading to metaphase arrest and inhibition of mitosis. At higher concentrations, Vincristine may disrupt and induce total depolymerization of microtubules. Vincristine induces apoptosis in tumor cells and inhibits SH-SY5Y cell proliferation with IC50 of 0.1 μM. Vincristine induces mitotic arrest and promots the expression of caspase-3 and -9 and cyclin B, while decreasing the expression of cyclin D. Vincristine induced neurotoxicity is caused by interference with microtubule function, which results in blockage of axonal transport and thus in axonal degeneration.


Cell Assay: Cells are plated in 2 mL of medium in 35-mm plates at a concentration of about 5 × 104 cells/mL and grow for 24 h at 37 ℃ in an atmosphere of 5% CO2 and 95% air. Then medium is replaced with fresh medium lacking or containing 4 nM drug and proliferation is continued for 3 days. Cell counts are done each day in a Coulter Counter after detaching the cells with trypsin and EDTA.

In VivoVincristine (3 mg/kg) administrated by a single i.p. injection to mice bearing bilateral subcutaneous xenografts Rh12 or Rh18, induces mean growth delay of>120 and>52 day, and repopulating fractions of 0.06% and 5%, respectively. Vincristine acts on subcutaneous colon 38 tumors in mice by host cell-mediated vascular effects as well as by direct tubulin-mediated cytotoxicity. Vincristine (5 mg/kg) reduces tumor blood flow of tumors by nearly 75%.
Animal modelHuman rhabdomyosarcoma xenografts Rh12
Formulation & DosageDissolved in water; 3 mg/kg; i.p. injection
ReferencesCancer Res. 1985 Jun;45(6):2741-7; Eur J Cancer. 1991;27(4):482-7.