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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVinblastine sulfateCat. No.: HY-13780CAS No.: 143-67-9Synonyms: Vincaleukoblastine sulfate salt分式: CHNOS分量: 909.05作靶点: Microtubule/Tubulin; Autophagy作通路: Cell Cycle/DNA Damage; Cytoskeleton; Autophagy储存式: 4C, protect from light*

2、 In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 44 mg/mL (48.40 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.1000 mL 5.5002 mL 11.0005 mL5 mM 0.2200 mL 1.1000 mL 2.2001 mL10 mM 0.1100 mL 0.5500 mL 1.1000 mL请根据产品在不同溶剂中

3、的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。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,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.75 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-C

4、D in saline)Solubility: 2.5 mg/mL (2.75 mM); Clear solution3. 请依序添加每种溶剂: 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (2.75 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Vinblastine sulfate种针对各种癌症类型的有细胞毒性的物碱。 长春花碱可抑制微管的形成,抑制nAChR的IC50值为8.9 M。IC50 & Target I

5、C50: 8.9 M(nAChR) 1体外研究 Vinblastine does not depolymerize spindle microtubules, yet it powerfully blocks mitosis (for example, IC500.8 nM in HeLa cells) and cells die by apoptosis 2. In NB4 cells, vinblastine produces alteration of p53 andDNA fragmentation. Vinblastine treatment has an antiprolifera

6、tive effect via the induction of apoptosisproducing Bax/Bcl-2 imbalance. Vinblastine treatment suppresses NFB expression and depresses NFB-DNA binding activity while maintaining JNK activation that subsequently results in apoptotic responsethrough caspase-dependent pathway 3. Vinblastine is found to

7、 trigger apoptosis as evidenced by the loss ofmitochondrial membrane potential, the release of both cytochrome c and apoptosis inducing factor, activationof caspase-9 and 3, and cleavage of Poly (ADP-ribose)-Polymerase 4.体内研究 Vinblastine is a widely used anticancer drug with undesired side effects.

8、Its conjugation with carriermolecules could be an efficient strategy to reduce these side effects 5.户使本产品发表的科研献 Mutat Res Genet Toxicol Environ Mutagen. 2016 Sep 15;808:27-37. Int J Clin Exp Pathol. 2017;10(3):3033-3042.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. McKay DB,

9、et al. Nicotinic and nonnicotinic receptor-mediated actions of vinblastine. Proc Soc Exp Biol Med. 1993 Jul;203(3):372-6.2. Pandya P, et al. Molecular recognition pattern of cytotoxic alkaloid vinblastine with multiple targets. J Mol Graph Model. 2014 Nov;54:1-9.3. Calvio E, et al. JNK and NFB depen

10、dence of apoptosis induced by vinblastine in human acute promyelocytic leukaemia cells. CellBiochem Funct. 2015 Jun;33(4):211-9.4. Selimovic D, et al. Vinblastine-induced apoptosis of melanoma cells is mediated by Ras homologous A protein (Rho A) via mitochondrialand non-mitochondrial-dependent mechanisms. Apoptosis. 2013 Aug;18(8):980-97.5. Bnczi Z, et al. Synthesis and in vitro antitumor effect of vinblastine derivative-oligoarginine conjugates. Bioconjug Chem. 2010 Nov17;21(11):1948-55.McePdfHeightCaution: Product has not been

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