硫酸長春新堿作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetVincristine sulfateCat. No.: HY-N0488CAS No.: 2068-78-2分式: CHNOS分量: 923.04作靶點(diǎn): Microtubule/Tubulin; Apoptosis作通路: Cell Cycle/DNA Damage; Cytoskeleton; Apoptosis儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 82.5 mg/mL (8

2、9.38 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲存時(shí)，請?jiān)?/p>

3、 6 個(gè)內(nèi)使，-20C 儲存時(shí)，請?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (2.98 mM); Clear sol

4、ution此案可獲得 2.75 mg/mL (2.98 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 27.5 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (2.98 mM); Clear solution此案可獲得 2.75 mg/mL (2.98 mM，飽和度未知) 的澄清溶液。以 1 mL

5、作液為例，取 100 L 27.5 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。Page 1 of 2 www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (2.98 mM); Clear solution此案可獲得 2.75 mg/mL (2.98 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 27.5 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGIC

6、AL ACTIVITY物活性 Vincristine sulfate種抗腫瘤長 花物堿，抑制有絲分裂紡錘體中的 microtubule 形成，導(dǎo)致中期階段的分裂細(xì)胞停滯。 它與 microtubule 結(jié)合的 Ki 為85 nM。體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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