水仙环素 TQ0183

Product Introduction
Bioactivity


英文名: Narciclasine

描述: Narciclasine (Lycoricidinol) 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。

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].

体外活性: Narciclasine在人脑胶质瘤多形性细胞中激活Rho和应力纤维（平均IC50约为50 nM，针对6种人脑胶质瘤多形性）。Narciclasine在一组60种癌细胞系中的平均IC50值为47 nM [1]。对于Narciclasine，其在根尖生长抑制的IC50测量值为0.1 μM [2]。

体内活性: 静脉注射Narciclasine，剂量为每千克体重1毫克，显著提高了携带GL19恶性胶质瘤小鼠的存活率。以相同剂量，每周五次，连续五周口服Narciclasine也显著提高了该模型中动物的存活率。以每千克体重1毫克的剂量口服Narciclasine，显著提高了携带Hs683恶性胶质瘤小鼠的存活率。增加每周给药次数并未提高这些携带Hs683恶性胶质瘤小鼠的存活率[1]。

存储条件: 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)


关键字: Rho-associated kinase | ROCK | inhibit | Inhibitor | ROK | Rho-associated protein kinase | Narciclasine | Rho-kinase

相关产品: 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

相关库: Rare Natural Product Library

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