Salirasib
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Salirasib(S-trans,trans-farnesylthiosalycilic acid [FTS])是合成的小分子Ras抑制剂[1]。
Ras家族传递胞外信号,由细胞表面受体起始,参与调节各种细胞过程,包括细胞生长、分化、运动性和细胞死亡。Ras信号的活化诱导多种受体的激活。 在许多癌症中,Ras信号处于活化状态[2]。
Salirasib的结构类似于Ras蛋白的羧基末端farnesylcysteine carboxy?methyl ester,作为锚固识别单元的一部分,驱逐细胞膜上的活性Ras蛋白。Salirasib很容易被细胞吸收,一旦进入细胞内可以特异性扰乱细胞膜内表面以及其它胞内膜上所有活化状态的Ras蛋白(H-ras、K-ras和N-ras)[1]。
已测定在胰腺癌细胞系和肿瘤异种移植模型中salirasib的活性。在Panc-1细胞系中,salirasib以剂量依赖性的方式降低Ras的量,25到50 μM可将Ras的含量最大程度的减少约50%。在小鼠肿瘤异种移植模型中,salirasib抑制Panc-1肿瘤的生长,与gemcitabine具有协同作用,均可抑制肿瘤生长,延长小鼠存活时间。Salirasib在实体瘤患者中进行临床I期试验,每日两次,给药21天,剂量分别为100、200、400、600 和800 mg,未达到毒性剂量限制,但800毫克的三个病人有1-2级腹泻,阻碍进一步的剂量递增治疗。II期临床研究推荐剂量为600 mg[3]。
参考文献:
[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.
2. Zeng M, Zhang B, et al. "Adenosine Attenuates LPS-Induced Cardiac Dysfunction by Inhibition of Mitochondrial Function via the ER Pathway." Evid Based Complement Alternat Med. 2019 Jan 10;2019:1832025. PMID:30733807
Storage | Store at -20°C |
M.Wt | 358.54 |
Cas No. | 162520-00-5 |
Formula | C22H30O2S |
Synonyms | S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS |
Solubility | insoluble in H2O; ≥16.2 mg/mL in EtOH; ≥16.75 mg/mL in DMSO |
Chemical Name | 2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienyl]sulfanylbenzoic acid |
SDF | Download SDF |
Canonical SMILES | CC(=CCCC(=CCCC(=CCSC1=CC=CC=C1C(=O)O)C)C)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
描述 | Salirasib是异戊烯化蛋白甲基转移酶(PPMTase)的抑制剂,Ki值为2.6 ?M。 | |||||
靶点 | PPMTase | |||||
IC50 | 2.6 ?M |
质量控制和MSDS
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