硫酸长春碱 T1668

Product Introduction
Bioactivity


英文名: Vinblastine sulfate

描述: Vinblastine sulfate (Vincaleukoblastine sulfate salt) 是对各种癌症类型有细胞毒性的生物碱。 它可以抑制微管的形成，也可以抑制 nAChR，IC50值为8.9 μM。

细胞实验: Six-well treatment plates are set up that contained 5 × 104 cells/mL in each well, suspended in 3 mL culture medium, and these are treated with vinblastine for 3 h followed by 21 h growth. (Only for Reference)

激酶实验: Cell based receptor autophosphorylation assays: Autophosphorylation of PDGFR family kinase assays are cell-based enzyme-linked immunosorbent (ELISA) assays using CHO cells expressing wild-type PDGFRβ, chimeric protein PDGFRβ/c-Kit, and PDGFRβ/Flt3 which contain the extracellular and transmembrane domains of PDGFRβ and the cytoplasmic domain of c-Kit, and Flt-3. Cells are grown to confluency in 96-well microtiter plates under standard tissue culture conditions, followed by serum starvation for 16 hours. Briefly, quiescent cells are incubated at 37 °C with increasing concentrations of Tandutinib for 30 minutes followed by the addition of 8 nM PDGF-BB for 10 minutes. Cells are lysed in 100 mM Tris, pH 7.5, 750 mM NaCl, 0.5% Triton X-100, 10 mM sodium pyrophosphate, 50 mM NaF, 10 μg/mL aprotinin, 10 μg/mL leupeptin, 1 mM phenylmethylsulfonyl fluoride, 1 mM sodium vanadate, and the lysate is cleared by centrifugation at 15,000 g for 5 minutes. Clarified lysates are transferred into a second microtiter plate in which the wells are previously coated with 500 ng/well of 1B5B11 anti-PDGFRβ mAb and then incubated for 2 hours at room temperature. After washing three times with binding buffer (0.3% gelatin, 25 mM HEPES, pH 7.5, 100 mM NaCl, 0.01% Tween 20), 250 ng/mL of rabbit polyclonal anti-phosphotyrosine antibody is added and plates are incubated at 37 °C for 60 minutes. Subsequently, each well is washed three times with binding buffer and incubated with 1 μg/mL of horseradish peroxidase-conjugated anti-rabbit antibody at 37 °C for 60 minutes. Wells are washed prior to adding 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid), and the rate of substrate formation is monitored at 650 nm.

体外活性: The average terminal half-lives of Vinblastine is 14.3 h. When incubated in freshly isolated rat hepatocytes, VLB penetrates rapidly and intensely into the cells, probably through a passive diffusion mechanism followed by tight cellular binding[3]. Vinblastine inhibits the angiogenic response induced by adrenomedullin and is also positive for mitotic slippage, causing micronuclei in mononucleate cells with cytokinesis block[4]. vinblastine gives significant increase in micronucleated mononucleated cells at concentrations that produced approximately 50% cell death and cytostasis or less as calculated using RPD, RICC and RCC[2].

体内活性: Vinblastine is a widely used anticancer drug with undesired side effects [6]. A combination of VBL and RAP at very low doses against human HCC gets a satisfactory antiangiogenic effect in vivo[4]. The clinically relevant dose of vinblastine inhibits palmitoylation of tubulin in vivo in CEM cells (effect on depalmitoylation of tubulin)[5].

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 90.9 mg/mL(100 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | Vinblastine sulfate | Vincaleukoblastine | Autophagy | Vincaleukoblastine Sulfate | Microtubule/Tubulin | Inhibitor | Vinblastine Sulfate | NSC 49842 | Vinblastine | NSC-49842

相关产品: Maytansinol | Lys-SMCC-DM1 | Tubulin inhibitor 7 | MMAF | CMPF | Deoxypodophyllotoxin | 10-Deacetyltaxol | GSK-3 inhibitor 3 | Tubulin inhibitor 35 | Entasobulin

相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Cancer Drug Library | Microtubule-Targeted Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Traditional Chinese Medicine Monomer Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library

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