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CAS No.: 162520-00-5

法尼基硫代水杨酸 Catalog No. CSN16117

Synonyms: S-Farnesylthiosalicylic acid;Farnesyl Thiosalicylic Acid;FTS

Salirasib is an inhibitor of prenylated protein methyltransferase (PPMTase) with Ki of 2.6 μM and can inhibit the methylation of Ras.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PPMTase

Ki:2.6μM
描述The free carboxyl group of the terminal farnesylcysteine or geranylgeranylcysteine in a large number of prenylated proteins is methylated by the prenylated protein methyltransferase (PPMTase), a unique enzyme among methyltransferases and this enzyme tightly associates with the particulate fractions in eukaryotic cells. Ras proteins are members of a family of GTPases that are essential components of receptor-mediated signaling cascades which regulate cell growth and differentiation and are also important components of signaling pathways that regulate cell death, cell shape and cell motility. Salirasib (S-trans,trans-Farnesylthiosalicylic acid (FTS)), a novel farnesylated rigid carboxylic acid derivative, acts as a potent competitive inhibitor of PPMTase with K_i of 2.6 mM. Salirasib inhibited the growth of human Ha-ras-transformed Rat1 cells in vitro with EC₅₀ of 7.5 μM^[3]. In Panc-1 cells, FTS at a concentration of 25 – 100 mM reduced the amount of Ras in a dose-dependent manner^[4]. Daily FTS treatment (5 mg/kg intraperitoneally) in Panc-1 xenografted mice markedly decreased tumor growth (after treatment for 18 days, tumor volume had increased by only 23 ± 30-fold in the FTS-treated group and by 127 ± 66-fold in controls)^[4]. Salirasib reduced survivin expression in a time- and dose-dependent manner. After 48h of incubation with 150 mM of salirasib, mRNA levels of survivin decreased by 60, 70 and 45% in HepG2, Hep3B and Huh7, respectively^[5]. 9L gliosarcoma cells established tumor-bearing rats were treated with convection enhanced drug delivery (CED) of salirasib (50 μM), at 10 days, average tumor growth rates (normalized in each rat to the initial tumor volume and then averaged over the group of rats) was1.61 ± 0.32 in salirasib-treated rats compared with 3.22 ± 0.55 in control^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00531401	Carcinoma, Non-Small-Cell Lung	Phase 2	Completed	-	United States, New York ... more >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10017 Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7891 mL
- 13.9454 mL
- 27.8909 mL
- 5 mM
- 0.5578 mL
- 2.7891 mL
- 5.5782 mL
- 10 mM
- 0.2789 mL
- 1.3945 mL
- 2.7891 mL

技术信息

CAS号

162520-00-5

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H30O2S

运输

蓝冰

分子量

358.54

别名

S-Farnesylthiosalicylic acid;Farnesyl Thiosalicylic Acid;FTS;法尼基硫代水杨酸

溶解度

DMSO	225.0 mg/mL (627.5 mM)
Water	insoluble

动物实验配方

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法尼基硫代水杨酸 Catalog No. CSN16117

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