Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vinflunine Tartrate 是一种独特的新型长春花生物碱,具有抑制有丝分裂和微管蛋白相互作用活性的特性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | 待询 | 待询 | ||
2 mg | 待询 | 待询 | ||
5 mg | 待询 | 待询 | ||
10 mg | 待询 | 待询 | ||
25 mg | 待询 | 待询 | ||
50 mg | 待询 | 待询 | ||
1 mL * 10 mM (in DMSO) | 待询 | 待询 |
产品描述 | Vinflunine Tartrat is a vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity. |
体外活性 | The major effects of Vinflunine on dynamic instability are a slowing of the microtubule growth rate, an increase in growth duration, and a reduction in shortening duration. The effects of Vinflunine on the readmilling rate is examined by following [3H]GTP incorporation into MAP-rich microtubules, and the IC50 is 0.42 μM. [1] Vinflunine induced mitotic accumulation with IC50 with 18.8 nM, which decreases the centromere dynamicity by 44% and increases the time centromeres spent ina paused state by 63%. [2] Vinflunine ditartrate exhibits microtubule inhibition (purified tubulin and MTP) and cytotoxicity in L1210 cells with IC50 of (0.49 μM and 3.5 μM) and 97 nM, respectively. [3] Vinflunine induces apoptosis in neuroblastoma SK-N-SH cells through a postmitotic G1 arrest and a mitochondrial pathway in a concentration-dependent manner with an IC50 with 50 nM. sup>[4] Treatment of Vinflunine induces a rapid change in endothelial cell shape: cells retracts and assumes a rounded morphology. Mean IC50 values are 9.9 x 10-5 M x 10-5 M for fibronectin and 5.0x 10-5 M x 10-5 M for type IV collagen. A short 4 hours exposure of endothelial cells to Vinflunine at 10-8 |
体内活性 | Intravenous treatment of mice with Vinflunine, immediately before and 2 day after Matrigel implantation, results in a dose-dependent inhibition of the bFGF-induced angiogenic response, compared with vehicle-treated animals. Inhibition of haemoglobin content is significant at 1.25, 2.5 and 5 mg/kg, with no effect at 0.63 mg/kg (P > 0.05). An ID50 value (dose which inhibits 50% of bFGF-induced neovascularisation) is calculated as 1 mg/kg. Low doses of Vinflunine reduce the number of experimental liver metastases by human LS174T colon cancer cell. A slight overall decrease in liver metastatic foci is already observed at the very low dose of 0.16 mg/kg Vinflunine, although maximal overall inhibition is reached at the maximal tolerated dose (MTD) of 20 mg/kg. [5] |
激酶实验 | Determination of Microtubule Polymer Mass: Purified tubulin (17 μM) is polymerized into microtubules in the abence or presence of a range of vnflunine concentrations (35 minutes; 37 °C) in 75 mM PIPES, 1.8 mM MgCl2, 1.0 mM EGTA, and 1.5 mM GTP (pH 6.8) using sea urchin (Strongylocentrotus purpuratus) axonemes as seeds for assembly initiation. After incubation, polymerized microtubules are separated from unpolymerized tubulin by centrifugation (150,000 × g; 1 hour; 35 °C). The supernatant is aspirated, the sedimented microtubules are depolymerized in assembly buffer by incubation on ice (2 hours), and the protein content is determined. |
细胞实验 | Effects of Vinflunine on L1210 cell proliferation are determined using a standard growth inhibition assay. Exponentially growing L1210 cells (1.5 × 105 cells/well) in a 24-well plate are exposed to a range of concentrations of test compounds for 48 hours, prior to determining cell numbers using an electronic particle counter based on linear interpolation between data points.(Only for Reference) |
分子量 | 967.02 |
分子式 | C45H54F2N4O8·xC4H6O6 |
CAS No. | 1201898-17-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (46.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.0341 mL | 5.1705 mL | 10.341 mL | 25.8526 mL |
5 mM | 0.2068 mL | 1.0341 mL | 2.0682 mL | 5.1705 mL | |
10 mM | 0.1034 mL | 0.5171 mL | 1.0341 mL | 2.5853 mL | |
20 mM | 0.0517 mL | 0.2585 mL | 0.5171 mL | 1.2926 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Vinflunine Tartrate 1201898-17-0 Cytoskeletal Signaling Microtubule Associated Inhibitor inhibitor inhibit