Product Introduction
Bioactivity


英文名: Narciclasine

描述: Narciclasine (Lycoricidinol) 是一種植物生長調(diào)節(jié)劑。它通過調(diào)節(jié)Rho/Rho 激酶/LIM 激酶/cofilin 信號傳導(dǎo)途徑，大大增加GTP 酶RhoA 活性以及以RhoA 依賴性方式誘導(dǎo)肌動蛋白應(yīng)力纖維形成。

細(xì)胞實驗: 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].

動物實驗: 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].

體外活性: Narciclasine在人腦膠質(zhì)瘤多形性細(xì)胞中激活Rho和應(yīng)力纖維（平均IC50約為50 nM，針對6種人腦膠質(zhì)瘤多形性）。Narciclasine在一組60種癌細(xì)胞系中的平均IC50值為47 nM [1]。對于Narciclasine，其在根尖生長抑制的IC50測量值為0.1 μM [2]。

體內(nèi)活性: 靜脈注射Narciclasine，劑量為每千克體重1毫克，顯著提高了攜帶GL19惡性膠質(zhì)瘤小鼠的存活率。以相同劑量，每周五次，連續(xù)五周口服Narciclasine也顯著提高了該模型中動物的存活率。以每千克體重1毫克的劑量口服Narciclasine，顯著提高了攜帶Hs683惡性膠質(zhì)瘤小鼠的存活率。增加每周給藥次數(shù)并未提高這些攜帶Hs683惡性膠質(zhì)瘤小鼠的存活率[1]。

存儲條件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 25 mg/mL (81.37 mM)


關(guān)鍵字: Rho-associated kinase | ROCK | inhibit | Inhibitor | ROK | Rho-associated protein kinase | Narciclasine | Rho-kinase

相關(guān)產(chǎn)品: Chroman 1 | ZINC00881524 | ROCK2-IN-6 hydrochloride | ROCK-IN-6 | ROCK-IN-7 | SAR407899 | Akt/ROCK-IN-1 | GSK-25 | ROCK-IN-8 | AS 1892802

相關(guān)庫: Rare Natural Product Library

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