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Tipifarnib

CAS No. : 192185-72-1

MCE 國際站：Tipifarnib

產品活性：Tipifarnib (IND 58359) 抑制法尼基轉移酶 (FTase)，IC₅₀ 為 0.86 nM。Tipifarnib 具有潛在抗腫瘤和抗寄生蟲活性。

研究領域：Metabolic Enzyme/Protease

作用靶點：Farnesyl Transferase

In Vitro: Tipifarnib is a potent inhibitor of Trypanosoma Cruzi with the ED₅₀ of 4 nM.
Tipifarnib inhibits isolated human farnesyltransferase for a lamin B peptide and for the K-RasB peptide with IC₅₀ of 0.86 nM and 7.9 nM, respectively.
Tipifarnib shows inhibition of cell growth or angiogenesis, and induction of apoptosis in aggressive prostate cancer (PCa).
Tipifarnib (0.25 μM, 1?μM; 48 h) shows a significant decrease in the concentration of exosomes in C4-2B cells and PC-3 cells.
Tipifarnib (1?μM) significantly inhibits the protein concentration of Alix, nSMase2, and Rab27a in C4-2B cells.
Tipifarnib (0.25 μM) significantly inhibits the activation of p-ERK (downstream effector molecule of the Ras/Raf/ERK signaling pathway) but not total ERK in C4-2B and PC-3 cells.
Tipifarnib (1.25-5 μM; 30 min) promotes endoplasmic reticulum stress in U937 cells, resulting in dysregulation of intracellular calcium homeostasis.

In Vivo: Tipifarnib (10 mg/kg; ip; single dose) upregulated antiapoptotic protein, Bcl-xL in liver, and prevents mosue death induced by GalN/LPS.

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