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| 品牌 | absin | CAS | 162520-00-5 |
|---|---|---|---|
| 分子式 | C22H30O2S | 纯度 | 98% |
| 分子量 | 358.54 | 货号 | abs47028271 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a potent competitive prenylated prot | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Salirasib 162520-00-5
| 产品描述 | |
| 描述 | Salirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Phase 2. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 法尼基硫代水杨酸；S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS |
| 外观 | white to beige |
| 可溶性/溶解性 | 10 mM in DMSO |
| 生物活性 | |
| 靶点 | Ras |
| In vitro(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. |
| In vivo(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. 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. Salirasib (10 mg/kg, i.p.) inhibits tumour growth in a subcutaneous xenograft mice model without weight loss. |
| 参考文献 | |
| 参考文献 |
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| 研究领域 | |
| 研究领域 | CancerOncoproteins/suppressorsOncoproteinsSignal transducers CancerSignal transductionG protein signalingSmall G proteinsRas family CancerTumor biomarkersOncoproteins EpigeneticsTranscriptionCancer susceptibilityProto-oncogenes Signal TransductionSignaling PathwayG Protein SignalingSmall G ProteinsRas Family Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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