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