| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
| 100mg | 电议 |
Cell lines | Human leukemia cell line THP-1 |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | 100 ng/ml LPS plus 2 μM tipifarnib. 6 time points (0, 10, 20, 30, 40 and 50h) |
Applications | Tipifarnib showed significant inhibition of the cytokine/ MMP-9 production as early as 20 h for MCP-1 and IL-6 and 30 h for IL-1β and MMP-9. Tipifarnib showed no significant inhibition of IL-8 production. |
Animal models | Female BALB/c mice (6–7 weeks old) |
Dosage form | Tipifarnib was dissolved in 20% cyclodextran, and 50 mg/kg was orally administered to mice at 24, 17, and 1 h before intraperitoneal injection of 20 μg of LPS per mouse, 1 mg/kg. |
Applications | After treatment of 2h, tipifarnib significantly inhibited LPS-induced TNF-α production and inhibited 50% of MIP-1α and MCP-1 production. After 3h, tipifarnib inhibited about 50% of IL-6 production and almost complete inhibition of IL-1β production. IL12-p40 and -p70 induction by LPS was also inhibited by tipifarnib at 3 h, whereas IL-10 was not significantly changed at both time points. No effects of tipifarnib on LPS-induced KC were observed, consistent with in vitro results for IL-8. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| 产品描述 | Tipifarnib (also known as Zarnestra or R115777), an orally bioavailable quinolone analog of imidazole heterocyclics, is a potent and specific nonpeptidomimetic competitive inhibitor of farnesyltransferase (FTase), an enezyme mediating post-translational farnesylation of multiple protein substrates involved in tumor cell proliferation. It has demonstrated inhibition of growth and proliferation of a broad range of human tumor models (either wild-type or mutated RAS) via cytostatic rather than cytotoxic activity bothin vitroandin vivo. It cell-type dependently induces apoptosis in some neoplastic cell lineages other than acute myeloid leukemia (AML), including multiple myeloma (MM) cell lines and MM cultures from patients. Reference [1].P.K. Epling-Burnett and Thomas P. Loughran Jr. Suppression of farnesyltransferase activity in acute myeloid leukemia and myelodysplastic syndrome: current understanding and recommended use of tipifarnib. Expert Opin Investig Drugs. 2010; 19(5): 689-698 |
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