- Tipifarnib (Zarnestra)
| SalirasibInhibitor of active Ras protein |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.95%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
| Description | Salirasib is an inhibitor of prenylated protein methyltransferase (PPMTase) with Ki value of 2.6 µM. | |||||
| Targets | PPMTase | |||||
| IC50 | 2.6 µM | |||||
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| Cas No. | 162520-00-5 | SDF | Download SDF |
| Synonyms | S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS | ||
| Chemical Name | 2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienyl]sulfanylbenzoic acid | ||
| Canonical SMILES | CC(=CCCC(=CCCC(=CCSC1=CC=CC=C1C(=O)O)C)C)C | ||
| Formula | C22H30O2S | M.Wt | 358.54 |
| Solubility | ≥16.75 mg/mL in DMSO, ≥16.2 mg/mL in EtOH, <1.92 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Salirasib (S-trans,trans-farnesylthiosalycilic acid [FTS]) is a synthetic small molecule that acts as a potent Ras inhibitor.[1]
The Ras family of small GTPases transmits extracellular signals, which are initiated by cell-surface receptors and serve to regulate various cellular processes including cell growth, differentiation, motility and cell death. Signals transmitted by activated Ras induce activation of multiple effectors. Ras signaling is activated in a large number of human cancers. Mutations of codons 12, 13 and 61 in Ras result in constitutively active Ras, and activating mutations of the three major Ras isoforms (H, K and N) have been found in more than 33% of human cancers. [2]
Salirasib mimics the carboxy-terminal farnesylcysteine carboxymethyl ester common to all Ras proteins, which acts as part of a recognition unit for anchorage and dislodges the active Ras protein from the cell membrane. Salirasib is readily taken up by cells, and once inside the cell it specifically disrupts the association of active forms of all Ras proteins (H-ras, K-ras and N-ras) with the inner surface of the cell membrane and with other cellular membranes. [1]
The in vitro activity of salirasib has been demonstrated in pancreatic cell lines and xenograft models. In the Panc-1 cell line, salirasib decreased the amount of RAS in a dosedependent manner, with a maximum decrease in Ras of approximately 50 % seen at concentrations of 25 to 50 μM. In the mouse xenograft models, salirasib inhibites Panc-1 tumor growth and is shown to be synergistic with gemcitabine, both inhibiting tumor growth and prolonging survival. Salirasib is tested in a phase I study in patients with solid tumors twice daily for 21 days every 4 weeks. Doses are escalated from 100 to 200, 400, 600, and 800 mg. Dose-limiting toxicity is not reached, but all three patients treated with 800 mg experienced Grade 1–2 diarrhea, preventing further dose escalation. The recommended dose for phase II studies is 600 mg bid. [3]
References:[1] Ernesto Bustinza-Linares, Razelle Kurzrock , Apostolia-Maria Tsimberidou. Salirasib in the treatment of pancreatic cance. Future Oncol. (2010) 6(6), 885–891.[2] Sari Schokoroy, Dolly Juster, Yoel Kloog, Ronit Pinkas-Kramarski. Disrupting the Oncogenic Synergism between Nucleolin and Ras Results in Cell Growth Inhibition and Cell Death. PLOS ONESeptember 2013, Volume 8, Issue 9, e75269.[3] Daniel Laheru , Preeti Shah, N. V. Rajeshkumar et al. Integrated preclinical and clinical development of S-trans, trans-farnesylthiosalicylic acid (FTS, Salirasib) in pancreatic cancer. Invest New Drugs (2012) 30:2391–2399.
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大家miRNA逆转录和qPCR的试剂盒用的是那个公司的啊，求推荐！
加尾法是采用加A酶先对mirna进行加尾，然后再用带oligodt的引物反转录，他的反转录引物是通用的，一次反转录可以获得所有miRNA的cdna，效率高。茎环法是采用特异性反转录引物序列+颈环结构作为反转录引物进行反转录的，一次反转录只能获得一种mirna的cdna，可能有几种一起反转录的，这个我不太清楚一起反转录的效果。然后茎环法的经典即ABI的探针法定量试剂盒。我用过茎环法反转录+染料法定量的，下游引物为通用引物，结果不太好，就现在用的这家的他采用的是双向引物都是特异性的，效果还可以。不知道我说的清楚不，希望能对你有帮助。
1.模板提取（一般为RNA）：Trizol、氯仿、异丙醇、无水乙醇、DEPC处理水
2.模板浓度测定：分光光度计或NanoDrop
3.逆转录：逆转录试剂盒（或者一步法试剂盒），这一步可以用普通PCR做，也可以用水域做。
4.荧光定量PCR试剂：通常有用SYBR Green Mix做的，但是这里建议你用EvaGreen做，灵敏度和平行性都要好于SYBR Green，并且如果你那是ABI或者Stratagene的PCR如果用SYBR Green还需要加一步Rox很麻烦。
5.其他：除了以上的那些还需要离心管、PCR管或板（Axygen反应比较好）、移液枪等，暂时就想到这么多。
转录的只是插入的片断，怎么会跟模板一样大呢，一般情况下应该比模板小多了。我都是跑电泳，严格来说应该跑变性的；嫌麻烦可以非变性，快速（防止RNA降解）十分钟即可；抛出来的带会有两条，上面大的是模板，下面一条比较亮的是RNA，那么你的转录就 成功了。
PCR第一个步骤如果没记错的话应该叫“变性”， PCR的话是不需要解旋酶的，直接利用DNA的高温变性特性，在高温下，使氢键断开，DNA双链恢复为单链。 （还有解旋酶好像是解除双螺旋的结构，是一种拓扑异构酶，对于氢键的打开没有贡献吧
2.模板浓度测定：分光光度计或NanoDrop
3.逆转录：逆转录试剂盒（或者一步法试剂盒），这一步可以用普通PCR做，也可以用水域做。
4.荧光定量PCR试剂：通常有用SYBRGreenMix做的，但是这里建议你用EvaGreen做，灵敏度和平行性都要好于SYBRGreen，并且如果你那是ABI或者Stratagene的PCR如果用SYBRGreen还需要加一步Rox很麻烦。
5.其他：除了以上的那些还需要离心管、PCR管或板（Axygen反应比较好）、移液枪等，暂时就想到这么多。
