| 名称 | CP-609754 |
| 描述 | CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity. It inhibits farnesylation of recombinant human H-Ras (IC50=0.57 ng/mL) and K-Ras (IC50=46 ng/mL)[1]. In 3T3 H-ras (61L)-transfected cell lines, CP-609754 exhibits a slow on/off rate, inhibiting mutant H-Ras farnesylation with an IC50 of 1.72 ng/mL[1]. The compound is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI, selectively inhibiting farnesylation of both H- and K-Ras proteins in 3T3 transfectants[1]. In vivo, CP-609754 shows antitumor activity against 3T3 H-ras (61L) tumors, with tumor regression achieved at 100 mg/kg twice daily and an ED50 for tumor growth inhibition at 28 mg/kg[1]. Continuous i.p. infusion of CP-609754 inhibits tumor growth by over 50% and reduces tumor farnesyltransferase activity by over 30% when plasma concentration is maintained above 118 ng/mL[1].
[1]. Stacy L Moulder, et al. A phase I open label study of the farnesyltransferase inhibitor CP-609,754 in patients with advanced malignant tumors. Clin Cancer Res. 2004 Nov 1;10(21):7127-35. |
| 体外活性 | CP-609754 (CP-609,754) serves as a reversible farnesyltransferase inhibitor, characterized by a slow on/off rate, effectively inhibiting the farnesylation of mutant H-Ras in 3T3 H-ras (61L)-transfected cell lines with an IC50 of 1.72 ng/mL, as evidenced by SDS-PAGE analysis of [35S]methionine-labeled material[1]. The compound exhibits competitive inhibition toward the prenyl acceptor (H-Ras protein) while being noncompetitive relative to the prenyl donor, farnesyl PPI. It operates by engaging with the farnesyltransferase-farnesyl PPI complex and vying for H-Ras protein binding, demonstrating selective inhibition of both H- and K-Ras proteins' farnesylation in 3T3 transfectants[1]. |
| 体内活性 | CP-609754 exhibits antitumor activity in vivo against 3T3 H-ras (61L) tumors. Administration of CP-609754 orally twice daily leads to tumor regression at a dose of 100 mg/kg, and the effective dose for inhibiting 50% of tumor growth (ED50) is 28 mg/kg. Continuous intraperitoneal (i.p.) infusion of CP-609754 results in over 50% inhibition of tumor growth and more than 30% reduction in tumor farnesyltransferase activity in mice, provided the plasma concentration of CP-609754 remains above 118 ng/mL[1]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 100 mg/mL (208.35 mM), Sonication is recommended.
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| 关键字 | Malignant | farnesylation | Farnesyltransferase | Tumor | Inhibitor | LNK-754 | CP 609754 | H-Ras | Ftase | OSI 754 | CP-609754 | Farnesyl Transferase | LNK 754 | OSI-754 | inhibit | OSI754 | LNK754 | K-Ras | Advanced | CP609754 |
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| 相关库 | 经典已知活性库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 代谢化合物库 | 临床期小分子药物库 | 已知活性化合物库 | 抗癌化合物库 | 抗癌活性化合物库 | 抗癌药物库 |
United States
