CAS NO: | 1092521-74-8 |
包装 | 价格(元) |
5mg (solution) | 电议 |
10mg (solution) | 电议 |
50mg (solution) | 电议 |
Physical Appearance | A solution in ethanol. To change the solvent, simply evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice. |
Storage | Store at -20°C |
M.Wt | 357.6 |
Cas No. | 1092521-74-8 |
Formula | C22H31NOS |
Synonyms | FTS Amide,Salirasib Amide |
Solubility | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide |
Chemical Name | 2-[[(2E,6E)-3,7,11-trimethyl-2,6,10-dodecatrien-1-yl]thio]-benzamide |
Canonical SMILES | C\C(CC/C=C(CC/C=C(C)\C)\C)=C/CSC1=C(C(N)=O)C=CC=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。 |
IC50: 20 and 10 μM for the growth of PANC-1 and U87 tumor cells, respectively
Farnesyl thiosalicylic acid amide (FTS-A), an farnesyl thiosalicylic acid derivative, inhibits tumor growth.
Farnesylthiosalicylic acid (FTS, Salirasib), a Ras inhibitor, can interfer with Ras membrane interactions that are crucial for Ras-dependent transformation.
In vitro: Previous study examined the effects of the FTS-A and its two analogs (FTS-MA and FTS-DMA) on panc-1 and U87 cells and the results showed that all three FTS-amides caused a dose-dependent decrease in cell number of both cell lines exhibiting similar potencies. Cell death was observed at concentrations higher than 50 μM. The IC50s recorded in both cell lines were at the range of 10-20 μM. FTS-A, FTS-MA, and FTS-DMA caused a clear decrease in the levels of K-Ras-GTP in Panc-1 cells and in U87 cells. Reduction in the level of N-Ras-GTP was observed only in U87 cells and no effect on H-Ras-GTP was observed in either cell line [1].
In vivo: The effect of FTS-A on brain tumor growth was examined using a nude mouse model with human glioblastoma U87 cells intracranially implanted into the striatum area. FTS-A at 100 mg/kg was administered orally twice daily. Results showed that the increase in tumor volume recorded over time in the FTS-A treated mouse was significantly lower than that recorded in the control mouse. Moreover, it was found that more contrast agent molecules accumulated in the control mice as compared to the FTS-A treated mice. In addition, this study did not see any inflammatory response in the brains of the controls or in the brains of FTS-A-treated mice [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Goldberg, L. ,Haklai, R.,Bauer, V., et al. New derivatives of farnesylthiosalicylic acid (salirasib) for cancer treatment: Farnesylthiosalicylamide inhibits tumor growth in nude mice models. Journal of Medicinal Chemistry 52, 197-205 (2009).