Plinabulin|714272-27-2|-陌孚医药/Medlife

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Plinabulin

目录号: PL07229 纯度: ≥98.0%

CAS No. :714272-27-2

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中文名称	Plinabulin
中文别名	(3Z,6Z)-3-[(5-叔丁基-1H-咪唑-4-基)亚甲基]-6-(苯亚甲基)-2,5-哌嗪二酮;Plinabulin (NPI-2358) 抑制剂
英文名称	Plinabulin
英文别名	NPI 2358;Plinabulin (NPI-2358);(3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]piperazine-2,5-dione;NPI-2358;Plinabulin;PLINABULIN NPI-2358;3-(Z)-benzylidene-6-(((Z)-5-tert-butyl-1H-imidazol-4-yl)methylene)-piperazine-2,5-dione;KPU-2;Plinabulin [USAN:INN];Plinabulin, NPI2358,;Plinabulin, NPI2358, NPI-2358;S1176_Selleck;SureCN79095;-tert-butyl-1H-imidazol-4"tert-butyl-dehydrophenylahistin
Cas No.	714272-27-2
分子式	C₁₉H₂₀N₄O₂
分子量	336.39
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Plinabulin (NPI-2358) 是一种抗微管蛋白解聚的血管破坏剂，能结合 β-微管蛋白 (β-tubulin) 的秋水仙碱结合位点阻止聚合，并且对人肿瘤细胞系具有抑制作用，对 HT-29 细胞系的 IC₅₀ 值为 9.8 nM。

生物活性

Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC 50 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.

性状

Solid

IC50 & Target[1][2]

β-tubulin

体外研究(In Vitro)

Plinabulin (NPI-2358) (2-200 nM; 30 minutes; HUVECs cells) is a potent anti-tumor agent which is active in multidrug-resistant (MDR) tumor cell lines, and is able to rapidly induce tubulin depolymerization and monolayer permeability in HUVECs, 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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Plinabulin (0 mg/kg-15 mg/kg; intraperitoneal injection; female CDF1 and C3H/He mice) induces a time- and dose-dependent decrease in tumor perfusion. The KHT sarcoma is more sensitive than the C3H tumor to the anti-tumor effects of Plinabulin, while radiation response is enhanced in both models. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 50 mg/mL (148.64 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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