Vincristine-sulfate-Leurocristine-sulfate-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVincristine sulfateCat. No.: HY-N0488CAS No.: 2068-78-2Synonyms: Leurocristine sulfate; 22-Oxovincaleukoblastine sulfate分式: CHNOS分量: 923.04作靶點(diǎn): Microtubule/Tubulin作通路: Cell Cycle/DNA Damage; Cytoskeleton儲(chǔ)存式: 4C, protect from lig

2、ht* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 82.5 mg/mL (89.38 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)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(qǐng)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(chǔ)備液，

3、并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)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?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)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 solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solu

4、bility: 2.75 mg/mL (2.98 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (2.98 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Vincristine sulfate種抗腫瘤長(zhǎng) 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

5、外研究 Vincristine inhibits net addition of tubulin dimers at assembly ends of steady-state microtubules with Ki of 85nM 1. Vincristine stabilizes the spindle apparatus resulting in failure of the chromosomes to segregateleading to metaphase arrest and inhibition of mitosis at low concentrations. At hi

6、gher concentrations,Vincristine may disrupt and induce total depolymerization of microtubules 2. Vincristine induces apoptosis intumor cells and inhibits SH-SY5Y cell proliferation with IC50 of 0.1 M. Vincristine induces mitotic arrest andpromots the expression of caspase-3 and -9 and cyclin B, whil

7、e decreasing the expression of cyclin D3. Vincristine induced neurotoxicity is caused by interference with microtubule function, which results inblockage of axonal transport and thus in axonal degeneration 4.體內(nèi)研究 Vincristine (3 mg/kg, i.p.) induces mean growth delay of 120 and 52 day, and repopulate

8、s fractions of0.06% and 5%, 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 plates at a concentration of about 5104 cells/mL and grow for24 h at 37C in an atmosphere of 5% CO2 and 95% air. Th

9、en medium is replaced with fresh medium lackingor containing 4 nM drug and proliferation is continued for 3 days. Cell counts are done each day in a CoulterCounter after detaching the cells with trypsin and EDTA.MCE has not independently confirmed the accuracy of these methods. They are for referenc

10、e 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;10:939. Neurobiol Learn Mem. 2019 Jul 3:107038.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Jor

11、dan, M.A., et al. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cellproliferation in vitro. Cancer 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.

12、, et al, Action of the vinca alkaloids vincristine, vinblastine, and desacetyl vinblastine amide on axonal fibrillar organelles in2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEvitro. Cancer Res, 1977. 37(5): p. 1401-7.4. Horton, J.K., et al. Relationships between tumor responsiveness, vincristine

13、 pharmacokinetics and arrest of mitosis in human tumorxenografts. Biochem Pharmacol, 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 J Nanomedicine. 2017 Mar 16;12:2081-210