您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Narciclasine
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Narciclasine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Narciclasine图片
CAS NO:29477-83-6
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Lycoricidinol
水仙环素
产品介绍
Narciclasine是一种植物生长调节剂。它通过调节Rho/Rho 激酶/LIM 激酶/cofilin信号传导途径,大大增加GTP酶RhoA活性以及以RhoA依赖性方式诱导肌动蛋白应力纤维形成。

产品描述

Narciclasine, a natural product, modulates the Rho/Rho-kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity.

体外活性

Narciclasine activates Rho and stress fibers in glioblastoma multiforme cells (mean IC50: ~50 nM on the 6 human glioblastoma multiforme). The mean IC50 value of 47 nM for Narciclasine across a panel of 60 cancer cell lines [1]. The IC50 measured for radicle growth inhibition is 0.1 μM for Narciclasine [2].

体内活性

The i.v. regimen of Narciclasine at 1 mg/kg significantly increases the survival of GL19 glioblastoma multiforme-bearing mice. Narciclasine when given orally at the same dose five times a week for 5 consecutive weeks also significantly increases animal survival in this model. Oral treatment with Narciclasine at 1 mg/kg significantly increases the survival of Hs683 glioblastoma multiforme-bearing mice. Increasing the number of doses administered per week does not increase the survival of these Hs683 glioblastoma multiforme-bearing mice [1].

细胞实验

The Narciclasine IC50 concentration, the Narciclasine concentration that decreased by 50% the global growth rate of a given cell population, is assessed with the MTT assay. The cells are incubated for 72 h in the presence and absence of the Narciclasine (with concentrations ranging between 1 and 10000 nM concentrate) for the determination of Narciclasine IC50 values [1].

动物实验

The Hs683 cell line and GL19 primoculture grafted into the brains of nude immunodeficient mice both produced invasive brain tumors. Xenograft-bearing mice receive vehicle alone, oral temozolomide at 40 mg/kg (5 administrations per week for 5 consecutive weeks), or Narciclasine at 1 mg/kg either oral (once per week for 5 weeks) or i.v. (twice per week for 5 weeks). Drug administration is initiated respectively on days 5 and 7 post-tumor graftings for the Hs683 and GL19 models. The temozolomide dose and treatment schedule are selected based on previously optimized regimens. Narciclasine dose and treatment schedule are selected based on Narciclasine toxicity study in rats after oral administration and pharmacokinetic study that we have recently published. In toxicity study, Narciclasine (25, 10, or 1 mg/kg) is administered five times a week for 3 weeks and the no adverse effect level dose is defined to be 1 mg/kg/d p.o., with minimal acanthosis reactive changes and minor variations in some biochemistry parameters observed at this dose level considered to be nonadverse [1].

Cas No.

29477-83-6

分子式

C14H13NO7

分子量

307.26

别名

Lycoricidinol;水仙环素

储存和溶解度

DMSO:25 mg/mL (81.37 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years