硫酸长春新碱作用机制 - Medchemexpress - MCE中国

1、Product Data SheetVincristine sulfateCat. No.: HY-N0488CAS No.: 2068-78-2分式: CHNOS分量: 923.04作靶点: Microtubule/Tubulin; Apoptosis作通路: Cell Cycle/DNA Damage; Cytoskeleton; Apoptosis储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实验 DMSO : 82.5 mg/mL (8

2、9.38 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.0834 mL 5.4169 mL 10.8338 mL5 mM 0.2167 mL 1.0834 mL 2.1668 mL10 mM 0.1083 mL 0.5417 mL 1.0834 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 储存时，请在

3、 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (2.98 mM); Clear sol

4、ution此案可获得 2.75 mg/mL (2.98 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 27.5 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (2.98 mM); Clear solution此案可获得 2.75 mg/mL (2.98 mM，饱和度未知) 的澄清溶液。以 1 mL

5、作液为例，取 100 L 27.5 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。Page 1 of 2 www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (2.98 mM); Clear solution此案可获得 2.75 mg/mL (2.98 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 27.5 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGIC

6、AL ACTIVITY物活性 Vincristine sulfate种抗肿瘤长 花物碱，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。体外研究 Vincristine inhibits net addition of tubulin dimers at assembly ends of steady-state microtubules with Ki of 85 nM1. Vincristine stabilizes the spindle apparatus resulting in failu

7、re of the chromosomes to segregate leading tometaphase arrest and inhibition of mitosis at low concentrations. At higher concentrations, Vincristine may disruptand induce total depolymerization of microtubules2. Vincristine induces apoptosis in tumor cells and inhibits SH-SY5Y cell proliferation wit

8、h IC50 of 0.1 M. Vincristine induces mitotic arrest and promots the expression of caspase-3and -9 and cyclin B, while decreasing the expression of cyclin D3. Vincristine induced neurotoxicity is caused byinterference with microtubule function, which results in blockage of axonal transport and thus i

9、n axonal degeneration4.体内研究 Vincristine (3 mg/kg, i.p.) induces mean growth delay of 120 and 52 day, and repopulates fractions of 0.06% and5%, administrated in mice bearing bilateral subcutaneous xenografts Rh12 or Rh18, respectively5.PROTOCOLCell Assay 1 Cells are plated in 2 mL of medium in 35 mm

10、plates at a concentration of about 5104 cells/mL and grow for 24 h at37C in an atmosphere of 5% CO2 and 95% air. Then medium is replaced with fresh medium lacking or containing 4nM drug and proliferation is continued for 3 days. Cell counts are done each day in a Coulter Counter after detachingthe c

11、ells with trypsin and EDTA.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Eur J Med Chem. 2018 Feb 25;146:157-170. Int J Biol Macromol. 2019 Jan 30;128:574-582. Int J Nanomedicine. 2017 Mar 16;12:2081-2108. Front Microbiol. 2019 May 9;10:93

12、9. Front Oncol. 2020 Mar 13;10:308.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Jordan, M.A., et al. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro.Page 2 of 3 www.MedChemECa

13、ncer Res, 1985. 45(6): p. 2741-7.2. Gidding, C.E., et al, Vincristine revisited. Crit Rev Oncol Hematol, 1999. 29(3): p. 267-87.3. 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

14、(5): p. 1401-7.4. Horton, J.K., et al. Relationships between tumor responsiveness, vincristine pharmacokinetics and arrest of mitosis in human tumor xenografts. BiochemPharmacol, 1988. 37(20): p. 3995-4000.5. 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. 482-7.6. Zhang D, et al. Co-delivery nanoparticles with characteristics of intracellular precision release drugs for overcoming multidrug resistance. Int JNanomedicine. 2017 Mar 16;12:2081-210