Vincristine-d3-ester sulfate(Synonyms: Leurocristine-d3-ester sulfate; NSC-67574-d3-ester sulfate; 22-Oxovincaleukoblastine-d3-ester sulfate)

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Vincristine-d3-ester sulfate (Synonyms: Leurocristine-d3-ester sulfate; NSC-67574-d3-ester sulfate; 22-Oxovincaleukoblastine-d3-ester sulfate)

Vincristine-d3-ester (Leurocristine-d3-ester) sulfate 是 Vincristine sulfate 的氘代物。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 Ki 为85 nM。

Vincristine-d3-ester sulfate(Synonyms: Leurocristine-d3-ester sulfate; NSC-67574-d3-ester sulfate; 22-Oxovincaleukoblastine-d3-ester sulfate)

Vincristine-d3-ester sulfate Chemical Structure

CAS No. : 1217854-24-4

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生物活性

Vincristine-d3-ester (Leurocristine-d3-ester) sulfate is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1] .

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

926.05

Formula

C46H55D3N4O14S
CAS 号

1217854-24-4
中文名称

硫酸长春新碱 ester (硫酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Jordan, M.A., et al. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro. Cancer Res, 1985. 45(6): p. 2741-7.

    [3]. Gidding, C.E., et al, Vincristine revisited. Crit Rev Oncol Hematol, 1999. 29(3): p. 267-87.

    [4]. Donoso, J.A., et al, Action of the vinca alkaloids vincristine, vinblastine, and desacetyl vinblastine amide on axonal fibrillar organelles in vitro. Cancer Res, 1977. 37(5): p. 1401-7.

    [5]. Horton, J.K., et al. Relationships between tumor responsiveness, vincristine pharmacokinetics and arrest of mitosis in human tumor xenografts. Biochem Pharmacol, 1988. 37(20): p. 3995-4000.

    [6]. Baguley, B.C., et al, Inhibition of growth of colon 38 adenocarcinoma by vinblastine and colchicine: evidence for a vascular mechanism. Eur J Cancer, 1991. 27(4): p. 482-7.

    [7]. Zhang D, et al. Co-delivery nanoparticles with characteristics of intracellular precision release drugs for overcoming multidrug resistance. Int J Nanomedicine. 2017 Mar 16;12:2081-2108.

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