產品屬性:
產品名稱 | 規(guī)格 | CAS號 | 型號 |
CP-609754 | 5 mg 10 mg 25 mg | 1190094-64-4 | EY-Y0164550 |
Cas No.1190094-64-4
別名 N/A
化學名 N/A
分子式 C29H22ClN3O2
分子量 479.96
溶解度 DMSO : 100 mg/mL (208.35 mM; Need ultrasonic)
儲存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述:
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.
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關鍵字: 1190094-64-4;C29H22ClN3O2;CP-609754;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學、分子生物學和常規(guī)生化試劑等為一體的科研產品銷售企業(yè),公司自成立以來,秉承""全心全意服務于科研工作者""的企業(yè)理念,立足生物科技領域,運用生物技術和科研試劑,發(fā)展現(xiàn)代生物科技,為各類大中小醫(yī)院及其它醫(yī)療機構、高等院校、科研院所、企事業(yè)單位提供優(yōu)質的產品,服務生物科技領域的科學研究人員。
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