CAS:162520-00-5
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to yellow Solid
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SalirasibCAS:162520-00-5
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to yellow Solid
CAS | 162520-00-5 |
Chinese Name | 沙利雷塞 |
English Name | Salirasib |
Synonyms | 法尼基硫代水杨酸;Farnesylthiosalicylate;Farnesylthiosalicylicacid;Lopac-F-8175;Salirasib; |
Molecular Formula | C22H30O2S |
Molecular Weight | 358.54 |
Solubility | Soluble in DMSO |
Purity | ≥98% |
Appearance | White to yellow Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL | MFCD00467723 |
SMILES | O=C(O)C1=CC=CC=C1SC/C=C(C)/CC/C=C(C)/CC/C=C(C)/C |
Target Point | Ras |
Passage | Cell Cycle; GPCR & G Protein |
Background | It is a Ras inhibitor. |
Biological Activity | Salirasib是一种 Ras 抑制剂,可特异性抑制致癌激活的Ras和生长因子受体介导的Ras激活,从而抑制Ras依赖性肿瘤生长。[1-3] |
In Vitro | Salirasib(50,100,150μM)诱导HCC细胞中细胞生长的剂量和时间依赖性降低。 Salirasib通过调节细胞周期效应物和抑制剂来减少细胞增殖。 Salirasib诱导HepG2和Hep3B细胞凋亡。 salirasib在HCC细胞系中的生长抑制作用与mTOR抑制无关,与ERK或Akt活化无关[2]。Salirasib(12.5-100μM)以剂量依赖性方式抑制ELT3细胞的增殖,平均IC50为58.57±4.59μM。 Salirasib对TSC2-无效细胞的作用显然被DN-Rheb模拟,但不被DN-Ras模拟。 Salirasib减少TSC2缺失细胞中的Rheb,并且TSC2表达使细胞免于Salirasib的抑制作用。 Salirasib可降低TSC2无效ELT3细胞中S6K的磷酸化,但不会降低ERK的磷酸化[1]。 |
In Vivo | Salirasib(40,60或80 mg/kg,po)在体内以剂量依赖性方式显著抑制肿瘤生长[1]。 Salirasib(5 mg/kg,ip)显著降低dy2J/dy2Jmice中的Ras表达,并导致Ras表达的增加,这远远低于dy2J/dy2J小鼠中观察到的增加。 Salirasib治疗与dy2J/dy2J小鼠中MMP-2和MMP-9活性的显著抑制相关[2]。 Salirasib(10 mg/kg,ip)在皮下异种移植小鼠模型中抑制肿瘤生长而没有体重减轻[3]。 |
Cell Experiment | 对于时间依赖性反应研究,每天用0.05%胰蛋白酶-EDTA收获细胞1至7天,并使用台盼蓝排除法在显微镜下计数。对于剂量反应研究,将细胞在补充有salirasib或DMSO的培养基中孵育3天。根据制造商的说明,使用比色WST-1测定法测定细胞活力。 |
Animal Experiment | 将六周大的雌性无胸腺NMRI nu/nu小鼠圈养在过滤顶部的笼子中并随意接收食物和水。通过将12×小鼠中悬浮于100μLPBS中的5×106 HepG2细胞皮下注射到右下腹侧来产生肿瘤。细胞接种后两周,当可触知的肿瘤建立时,将小鼠分成salirasib处理的(n = 6)和对照组(n = 4)。两只动物在该时间点不发展肿瘤,必须从研究中排除。他们每天腹膜内注射10mg/kg salirasib或类似体积的载体溶液(含有2.5%v/v乙醇的PBS,pH8.0)12天。从治疗的第一天开始,用数字卡尺每周记录肿瘤尺寸三次。肿瘤体积估计如下:V(mm 3)=(长度×宽度2)/ 2。在处死时记录肿瘤重量以评估治疗反应。 |
Data Literature Source | [1]. Makovski V,et al. Farnesylthiosalicylic acid (salirasib) inhibits Rheb in TSC2-null ELT3 cells: a potential treatment for lymphangioleiomyomatosis. Int J Cancer. 2012 Mar 15;130(6):1420-9. [2]. Nevo Y,et al. Chapman J. The Ras antagonist,farnesylthiosalicylic acid (FTS),decreases fibrosis and improves muscle strength in dy/dy mouse model of muscular dystrophy. PLoS One. 2011 Mar 22;6(3):e18049. [3]. Charette N,et al. Salirasib inhibits the growth of hepatocarcinoma cell lines in vitro and tumor growth in vivo through ras and mTOR inhibition. Mol Cancer. 2010 Sep 22;9:256. |
Unit | Bottle |
Specification | 10mg 50mg |