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普那布林 /Plinabulin {[allProObj[0].p_purity_real_show]}

货号:A840538 同义名: NPI-2358

Plinabulin is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells.

Plinabulin 化学结构 CAS号:714272-27-2
Plinabulin 化学结构
CAS号:714272-27-2
Plinabulin 3D分子结构
CAS号:714272-27-2
Plinabulin 化学结构 CAS号:714272-27-2
Plinabulin 3D分子结构 CAS号:714272-27-2
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Plinabulin 纯度/质量文件 产品仅供科研

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Plinabulin 生物活性

靶点
  • VDA

    Tubulin, IC50:9.8 nM-18 nM

描述 Plinabulin (NPI-2358) acts as a vascular disrupting agent and inhibits tubulin depolymerization with an IC50 of 9.8 nM in HT-29 cells[1]. Plinabulin attaches to the colchicine binding site on β-tubulin, inhibiting its polymerization and exhibiting strong anti-tumor properties[2].
体内研究

Plinabulin, administered intraperitoneally at doses ranging from 0 mg/kg to 15 mg/kg to female CDF1 and C3H/He mice, results in a time- and dose-dependent reduction in tumor perfusion. KHT sarcoma exhibits a higher sensitivity to Plinabulin's anti-tumor effects compared to C3H tumors, with both models showing an enhanced response to radiation[3].

体外研究

Plinabulin (NPI-2358), in concentrations ranging from 2-200 nM and applied for 30 minutes to HUVECs cells, acts as a potent anti-tumor agent. It effectively induces tubulin depolymerization and increases monolayer permeability, showing activity against multidrug-resistant tumor cell lines with IC50 values of 18 nM for DU 145 cells, 13 nM for PC-3 cells, 14 nM for MDA-MB-231 cells, 18 nM for NCI-H292 cells, and 11 nM for Jurkat leukemia cells[1].

Plinabulin 参考文献

[1]Nicholson B et al. NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent. Anticancer Drugs. 2006 Jan;17(1):25-31.

[2]Monica M. Mita et al. Phase 1 First-in-Human Trial of the Vascular Disrupting Agent Plinabulin (NPI-2358) in Patients with Solid Tumors or Lymphomas Clin Cancer Res. 2010 Dec 1;16(23):5892-9.

[3]Bertelsen LB, et al. Vascular effects of plinabulin (NPI-2358) and the influence on tumour response when given alone or combined with radiation. Int J Radiat Biol. 2011 Nov;87(11):1126-34.

Plinabulin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.97mL

0.59mL

0.30mL

14.86mL

2.97mL

1.49mL

29.73mL

5.95mL

2.97mL

Plinabulin 技术信息

CAS号714272-27-2
分子式C19H20N4O2
分子量 336.388
别名 NPI-2358
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 50 mg/mL(148.64 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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