Home>>Signaling Pathways>> Cell Cycle/Checkpoint>> Microtubule/Tubulin>>Plinabulin (NPI-2358)

Plinabulin (NPI-2358) Sale

(Synonyms: 普那布林; NPI-2358) 目录号 : GC10235

A tubulin depolymerizing agent

Plinabulin (NPI-2358) Chemical Structure

Cas No.:714272-27-2

规格 价格 库存 购买数量
5mg
¥882.00
现货
10mg
¥1,796.00
现货
50mg
¥5,177.00
现货
200mg
¥15,099.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

产品描述

The IC50 values of NPI-2358 is 9.8 ± 2.4 nmol/l, 18 ± 5 nmol/l, 13 ± 1 nmol/l, 14 ± 2 nmol/l, 18 ± 1 nmol/l and 11 nmol/l for HT-29, DU 145, PC-3, MDA-MB-231, NCl-H292 and Jurkat cell lines, respectively[1].

Plinabulin (NPI-2358) is a vascular disrupting agent which binds to the colchicine-binding site of tubulin. NPI-2358 could destabilize tumor vascular endothelial architectural resulting in selective collapse of established tumor vasculature [1].

In vitro: NPI-2358 exhibited anti-tumor activity against various human tumor cell lines. In proliferating human umbilical vein endothelial cells (HUVECs), administration of NPI-2358 at 10 nmol/l induced tubulin depolymerization within 30 min [1]. In an in-vitro model of tumor vascular collapse, NPI-2358 increased HUVEC monolayer permeability in a dose-dependent manner. Plinabulin had also shown the in-vitro cytotoxic activity with IC50 values of 11 ± 5 nmol/l and 4.3 ± 2.2 nmol/l for MES-SA and HL-60 tumor cell lines, respectively[1].

In vivo: In the foot implanted C3H mammary carcinomas or leg implanted KHT sarcomas mice model, 7.5 mg/kg plinabulin (intraperitoneally injected) significantly reduced the transfer constant (K(trans)) and the initial area under curve (IAUC) within 1 hour after injection, reaching a lowest point at 3 h, but returning to normal within 24 h. A dose-dependent decrease in IAUC and K(trans) was seen at 3 h. 12.5 mg/kg and 1.5 mg/kg NPI-2358 showed significant anti-tumour effects in the C3H tumours and the KHT sarcoma, respectively .

Clinical trials: In patients evaluated at a dose of 30 mg/m², tumor blood flow (Ktrans) showed a 16% to 82% decrease. The half-life of NPI-2358 was 6.06 ± 3.03 hours, clearance was 30.50 ± 22.88 L/h, and distributive volume was 211 ± 67.9 L.

References:
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.

Chemical Properties

Cas No. 714272-27-2 SDF
别名 普那布林; NPI-2358
化学名 (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]piperazine-2,5-dione
Canonical SMILES CC(C)(C)C1=C(N=CN1)C=C2C(=O)NC(=CC3=CC=CC=C3)C(=O)N2
分子式 C19H20N4O2 分子量 336.39
溶解度 DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 1 mg/ml 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.9727 mL 14.8637 mL 29.7274 mL
5 mM 0.5945 mL 2.9727 mL 5.9455 mL
10 mM 0.2973 mL 1.4864 mL 2.9727 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置