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编 号:F434742
分子式:C19H20N4O2
分子量:336.39
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC50 of 9.8 nM against HT-29 cells. Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells.

体内研究:
PlinabuLin (0 mg/kg-15 mg/kg;腹膜内注射;雌性 CDF1 和 C3H/He 小鼠) 诱导肿瘤灌注的时间和剂量依赖性降低。KHT 肉瘤比 C3H 肿瘤对 Plinabulin 的抗肿瘤作用更敏感,而两种模型的放射反应均得到增强。Animal Model:Female CDF1 mice (10-14-week-old) with C3H mammary carcinoma; Female C3H/HeJ mice with KHT sarcoma cells (8-weeks-old)
Dosage:0 mg/kg, 1.5 mg/kg, 2.5 mg/kg, 5 mg/kg, 7.5 mg/kg, 10 mg/kg, 12.5 mg/kg, 15 mg/kg;0.02 mL/g mouse body weight in CDF1 mice and 0.01 mL/g body weight for C3H/HeJ mice
Administration:Intraperitoneal injection; 0 huor, 1 huor, 3 hours, 6 huors, 24 huors
Result:Induced a time- and dose-dependent decrease in tumour perfusion. The KHT sarcoma was more sensitive than the C3H tumour to the anti-tumor, while radiation response was enhanced in both models.

体外研究:
PlinabuLin (NPI-2358) (2 -200 nM;30 分钟;HUVECs 细胞) 是一种有效的抗肿瘤剂,在多重耐药 (MDR) 肿瘤细胞系中具有活性,能够快速诱导微管蛋白解聚和单层通透性在 HUVEC 中,DU 145 细胞的 IC50 值为 18 nM;PC-3 细胞为 13 nM;MDA-MB-231 细胞为 14 nM;NCI-H292 细胞为 18 nM;Jurkat 白血病细胞为 11 nM。
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