货号	规格	价格	上海	北京	珠海	重庆	武汉
S83728-5mg促销	≥98%	￥100.00 ￥80.00 S83728-5mg ￥80.00 2-3天	0 货期：2-3天	-	-	-	-
S83728-10mg促销	99.50%	￥145.00 ￥116.00 S83728-10mg ￥116.00 现货	5 5	-	-	-	-
S83728-25mg促销	99.50%	￥245.00 ￥220.00 S83728-25mg ￥220.00 现货	1 1	-	-	-	-
S83728-50mg	99.50%	￥400.00 S83728-50mg ￥400.00 现货	6 6	-	-	-	-
S83728-100mg	≥98%	￥640.00 S83728-100mg ￥640.00 2-3天	0 货期：2-3天	-	-	-	-
S83728-200mg	≥98%	￥1200.00 S83728-200mg ￥1200.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.

靶点：

Ki: 2.6 μM (PPMTase);Autophagy; Ras

体外研究：

Salirasib (12.5-100 μM) inhibits the proliferation of ELT3 cells in a dose-dependent manner with an average IC50 of 58.57±4.59 μM. The effects of Salirasib on the TSC2-null cells are evidently mimicked by DN-Rheb but not by DN-Ras. Salirasib reduces Rheb in TSC2-null cells and TSC2 expression rescues the cells from the inhibitory effect of Salirasib. Salirasib reduces phosphorylation of S6K but not of ERK in the TSC2-null ELT3 cells. Salirasib (50, 100, 150 μM) induces a dose- and time-dependent decrease of cell growth in HCC cells. Salirasib reduces cell proliferation through modulation of cell cycle effectors and inhibitors. Salirasib induces apoptosis in HepG2 and Hep3B cells. The growth inhibitory effect of salirasib in HCC cell lines is associated with mTOR inhibition independent of ERK or Akt activation

体内研究：

Salirasib (40, 60 or 80 mg/kg, p.o.) significantly inhibits the tumor growth in a dose dependent manner in vivo[1]. Salirasib (5 mg/kg, i.p.) significantly decreases Ras expression in the dy2J/dy2Jmice, and causes an increase in Ras expression which is by far much lower than the increase observed in the dy2J/dy2J mice. Salirasib treatment is associated with significantly inhibition of both MMP-2 and MMP-9 activities in the dy2J/dy2J mice[2]. Salirasib (10 mg/kg, i.p.) inhibits tumour growth in a subcutaneous xenograft mice model without weight loss

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.789 ml	13.945 ml	27.891 ml
5 mM	0.558 ml	2.789 ml	5.578 ml
10 mM	0.279 ml	1.395 ml	2.789 ml
50 mM	0.056 ml	0.279 ml	0.558 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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