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Tipifarnib(Zarnestra)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tipifarnib(Zarnestra)图片
CAS NO:192185-72-1
规格:98%
分子量:489.4
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
Farnesyltransferase inhibitor,potent and specific
CAS:192185-72-1
分子式:C27H22Cl2N4O
分子量:489.4
纯度:98%
存储:Store at -20°C

Background:

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
[2].Jean-Pierre Armand, Alan K. Burnett, Johannes Drach, Jean-Luc Harousseau, Bob Lowenberg and Jesus San Miguel. The emerging role of targeted therapy for hematologic malignancies: update on bortezomib and tipifarnib. The Oncologist 2007, 12:281-290
[3].Elzbieta Izbicka, David Campos, Gilbert Carrizales and Amita Patnaik. Biomarkers of anticancer activity of R115777 (tipifarnib, zarnestra) in human breast cancer models in vitro. Anticancer Research 2005; 25: 3215-3224