Plinabulin (NPI-2358)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NPI-2358对HT-29、DU 145、PC-3、MDA-MB-231、NCl-H292和Jurkat细胞系的IC50值分别是9.8 ± 2.4 nmol/l、18 ± 5 nmol/l、13 ± 1 nmol/l、14 ± 2 nmol/l、18 ± 1 nmol/l和11 nmol/l [1]。
Plinabulin(NPI-2358)是血管破坏剂,通过结合微管蛋白的秋水仙碱结合位点发挥作用。NPI-2358能够使肿瘤血管内皮不稳定,从而选择性的破坏已建立的肿瘤血管系统[1]。
体外实验:NPI-2358对多种人类肿瘤细胞系均显示抗肿瘤活性。在增殖的人脐静脉内皮细胞(HUVECs)中,10 nmol/l的NPI-2358施用30分钟内,NPI-2358诱导微管蛋白解聚[1]。在肿瘤血管闭塞的体外模型中,NPI-2358以剂量依赖的方式增加HUVEC的单层渗透性。Plinabulin还表现出体外细胞毒性,对MES-SA和HL-60肿瘤细胞系的IC50值分别为11 ± 5 nmol/l 和4.3 ± 2.2 nmol/l[1]。
在体实验:在足部植入C3H乳腺肿瘤或腿部植入KHT肉瘤小鼠模型中,腹腔注射7.5 mg/kg的plinabulin 1小时后,转移常数(K(trans))以及曲线下起始面积(IAUC)显著减少,并在3小时后达到最低点,但在24小时内恢复常态。12.5 mg/kg和1.5mg/kg的NPI-2358分别对于C3H肿瘤和KHT肉瘤表现出显著的抗肿瘤作用。
临床试验:在肿瘤患者中评估30 mg/m2的NPI-2358,肿瘤血流(Ktrans)下降16%到82%。 NPI-2358的半衰期为6.06 ± 3.03小时,清除率为30.50 ± 22.88 L/h,分布容积为211 ± 67.9 L.
参考文献:
Nicholson B1, Lloyd GK, Miller BR, Palladino MA, Kiso Y, Hayashi Y, Neuteboom ST. 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.
Bertelsen L B, Shen Y Y, Nielsen T, et al. Vascular effects of plinabulin (NPI-2358) and the influence on tumour response when given alone or combined with radiation[J]. International journal of radiation biology, 2011, 87(11): 1126-1134.
Millward M, Mainwaring P, Mita A, et al. Phase 1 study of the novel vascular disrupting agent plinabulin (NPI-2358) and docetaxel[J]. Investigational new drugs, 2012, 30(3): 1065-1073.
Storage | Store at -20°C |
M.Wt | 336.39 |
Cas No. | 714272-27-2 |
Formula | C19H20N4O2 |
Solubility | Soluble in DMSO |
Chemical Name | (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]piperazine-2,5-dione |
SDF | Download SDF |
Canonical SMILES | CC(C)(C)C1=C(N=CN1)C=C2C(=O)NC(=CC3=CC=CC=C3)C(=O)N2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | Plinabulin (NPI-2358), a vascular disrupting agent (VDA), is an inhibitor of tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. | |||||
Targets | Tubulin | |||||
IC50 | 9.8 nM-18 nM |