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CP-609754

CAS No. : 1190094-64-4

MCE 站：CP-609754

产品活性：CP-609754 (LNK-754) 是一种有效且可逆的法尼基转移酶(farnesyltransferase) 抑制剂，具有潜在的抗癌活性。CP-609754 抑制重组人 H-Ras 和重组 K-Ras法尼基化的 IC₅₀ 分别为 0.57 ng/mL 和 46 ng/mL。

研究领域：Metabolic Enzyme/Protease

作用靶点：Farnesyl Transferase

In Vitro: CP-609754 (CP-609,754) is a reversible inhibitor of farnesyltransferase with a slow on/off rate. CP-609,754 inhibits farnesylation (IC₅₀=1.72 ng/mL) of mutant H-Ras in 3T3 H-ras (61L)-transfected cell lines with SDS-PAGE analysis of [³⁵S]methionine-labeled material.
CP-609754 is competitive for the prenyl acceptor (H-Ras protein) ａnd noncompetitive for the prenyl donor farnesyl PPI. CP-609754 interacts with the farnesyltransferase-farnesyl PPI complex ａnd competes for the binding of the Ras protein. CP-609754 selectively inhibits farnesylation of both H- ａnd K-Ras proteins in 3T3 transfectants.

In Vivo: CP-609754 (CP-609,754) has antitumor activity against 3T3 H-ras (61L) tumors in vivo.
With twice daily oral dosing of CP-609754, tumor regression is achieved with a dose of 100 mg/kg; the ED₅₀ for tumor growth inhibition is 28 mg/kg.
With continuous i.p. infusion of CP-609754, tumor growth is inhibited by >50%, ａnd tumor farnesyltransferase activity inhibited by >30% in mice in which the plasma concentration of CP-609754 is maintained above 118 ng/mL.

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