LB42708
产品编号:Bellancom-15879| CAS NO:226929-39-1| 分子式:C30H27BrN4O2| 分子量:555.47
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LB42708
产品介绍 | LB42708 是一种有效的、选择性的和具有口服活性的法尼基转移酶 (farnesyltransferase)抑制剂。 LB42708 抑制 H-Ras、N-Ras 和 K-Ras4B 的法尼基化,IC50 分别为 0.8 nM、1.2 nM 和 2.0 nM。 | |||||||||
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生物活性 | LB42708 is a potent, selective and orally active farnesyltransferase inhibitor. LB42708 inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC50s of 0.8 nM, 1.2 nM and 2.0 nM, respectively. | |||||||||
体外研究 |
LB42708 induces cell death despite K-ras prenylation. Growth inhibition by LB42708 is accompanied by G1 and G2/M cell cycle arrests in H-ras and K-ras-transformed RIE cells, respectively. LB42708 induces the upregulation of p21(CIP1/WAF1) and RhoB above the basal level that leads to the cell cycle arrest and to distinct morphological alterations of ras-transformed rat intestinal epithelial (RIE) cells. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | |||||||||
体内研究 | ||||||||||
体内研究 | ||||||||||
性状 | Solid | |||||||||
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运输条件 | Room temperature in continental US; may vary elsewhere. | |||||||||
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