Salirasib
發(fā)布者：信康 瀏覽次數(shù)：
產(chǎn)品名稱:SalirasibCAS:162520-00-5別名：反,反法尼基硫代水楊酸(SALIRASIB);2-(((2E,6E)-3,7,11-三甲基十二碳-2,6,10-三烯-1-基)硫基)苯甲酸;2-[[(2E,6E)-3,7,11-三甲基-2,6,10-十二烷三烯-1-基]硫代]苯甲酸;反,反法尼基硫代水楊酸;沙利雷塞英文名：Salirasib
- 熔點 64-66°C
- 密度 1.05
- 儲存條件 -20°C Freezer
- 溶解度 DMSO: soluble20mg/mL, clear
- 顏色white to beige
- 生物活性Salirasib是一種有效的競爭性prenylated protein methyltransferase (PPMTase)抑制劑， Ki為2.6 μM，其抑制Ras甲基化。Phase 2。
- 體外研究Salirasib inhibits the growth of human Ha-ras-transformed Rat1 cells, which correlates well with their inhibition for PPMTase. Salirasib inhibits Ras methylation in Rat-1 fibroblasts, Ras-transformed Rat-1, and B16 melanoma cells. Salirasib also reduces the levels of Ras in cell membranes and inhibits Ras-dependent cell growth, independently of methylation, but via modulation of Ras-Raf communication. In Ras-transformed EJ cells, Salirasib interferes with the activation of Raf-1 and MAPK and inhibits DNA synthesis.
- 體內(nèi)研究In Panc-1 xenografted nude mice, Salirasib (5 mg/kg i.p.) markedly inhibits tumor growth without systemic toxicity. In male Wistar rats, Salirasib (5 mg/kg i.p.) markedly inhibits thioacetamide-induced -induced liver cirrhosis. In the dy(2J)/dy(2J) mouse model of congenital muscular dystrophy, Salirasib (5 mg/kg i.p.) attenuates fibrosis and improves muscle strength.
