购物车
- 全部删除
- 您的购物车当前为空
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。
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 | 库存 | 数量 |
---|---|---|---|
1 mg | 询价 | 期货 | |
2 mg | 询价 | 期货 | |
5 mg | 询价 | 期货 | |
10 mg | 询价 | 期货 | |
25 mg | 询价 | 期货 | |
50 mg | 询价 | 期货 | |
1 mL x 10 mM (in DMSO) | 询价 | 期货 |
产品描述 | Vinflunine Tartrate, a uniquely fluorinated vinca alkaloid, exhibits mitotic-arresting and tubulin-interacting properties. |
体外活性 | Vinflunine对微管动态不稳定性的主要影响包括微管生长速率的减缓、生长持续时间的增加以及缩短持续时间的减少。通过跟踪[3H]GTP合并到富含MAP的微管中来检查Vinflunine对重铣速率的影响,其IC50为0.42 μM。[1] Vinflunine引发的有丝分裂积累的IC50为18.8 nM,它通过降低着丝点的动态性44%并增加着丝点处于暂停状态的时间63%。[2] Vinflunine ditartrate显示对微管的抑制(纯化的tubulin和MTP)以及对L1210细胞的细胞毒性,其IC50分别为(0.49 μM和3.5 μM)和97 nM。[3] Vinflunine通过后有丝分裂G1阻滞和线粒体途径以浓度依赖性方式在神经母细胞瘤SK-N-SH细胞中诱导凋亡,IC50为50 nM。[4] Vinflunine处理导致内皮细胞形状迅速变化:细胞收缩并呈现圆形形态。对于纤维连接蛋白和IV型胶原蛋白,平均IC50值分别为9.9 x 10^-5 M和5.0 x 10^-5 M。短暂地将内皮细胞暴露于10^-8至10^-4 M的Vinflunine中,可抑制内皮细胞对NIH3T3细胞衍生的血管生成因子的运动反应。抑制作用呈剂量依赖性,平均IC50值为7.1 x 10^-7 M。[5] |
体内活性 | 小鼠经静脉给予Vinflunine治疗,具体时点为Matrigel植入前即刻以及之后2天,可见到对bFGF诱发的血管生成反应的剂量依赖性抑制。在1.25、2.5和5 mg/kg的剂量下,Vinflunine 对血红蛋白含量的抑制显著,而在0.63 mg/kg的剂量下无效(P > 0.05)。Vinflunine的低剂量能减少由人类LS174T结肠癌细胞引起的实验性肝转移数量。在极低剂量0.16 mg/kg Vinflunine下即可观察到肝转移灶的轻微总体减少,尽管在最大耐受剂量(MTD)20 mg/kg时达到最大总体抑制。[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) |
别名 | 长春氟宁酒石酸盐 |
分子量 | 967.02 |
分子式 | C45H54F2N4O8·xC4H6O6 |
CAS No. | 1201898-17-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 45 mg/mL (46.5 mM) | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.