Vincristine硫酸长春新碱,2068-78-2

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Vincristine sulfate

CAS No. : 2068-78-2

MCE 国际站：Vincristine sulfate

产品活性：Vincristine sulfate是一种抗肿瘤长春花生物碱，抑制有丝分裂纺锤体中的 microtubule 形成，导致中期阶段的分裂细胞停滞。 它与 microtubule 结合的 K_i 为85 nM。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  Apoptosis

作用靶点：Microtubule/Tubulin  |  Apoptosis

In Vitro: Vincristine inhibits net addition of tubulin dimers at assembly ends of steady-state microtubules with K_i of 85 nM. Vincristine stabilizes the spindle apparatus resulting in failure of the chromosomes to segregate leading to metaphase arrest and inhibition of mitosis at low concentrations. 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.

In Vivo: Vincristine (3 mg/kg, i.p.) induces mean growth delay of > 120 and > 52 day, and repopulates fractions of 0.06% and 5%, administrated in mice bearing bilateral subcutaneous xenografts Rh12 or Rh18, respectively.

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