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CP-609754 Sale

(Synonyms: LNK-754; OSI-754) 目录号 : GC62276

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。

CP-609754 Chemical Structure

Cas No.:1190094-64-4

规格 价格 库存 购买数量
5 mg
¥2,250.00
现货
10 mg
¥3,600.00
现货
25 mg
¥7,650.00
现货

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产品描述

CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL[1].

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[1].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[1].

CP-609754 (CP-609,754) has antitumor activity against 3T3 H-ras (61L) tumors in vivo[1].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[1]. 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[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.

Chemical Properties

Cas No. 1190094-64-4 SDF
别名 LNK-754; OSI-754
分子式 C29H22ClN3O2 分子量 479.96
溶解度 DMSO : 100 mg/mL (208.35 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.0835 mL 10.4175 mL 20.8351 mL
5 mM 0.4167 mL 2.0835 mL 4.167 mL
10 mM 0.2084 mL 1.0418 mL 2.0835 mL
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