LB42708
目录号: PL13911
CAS No. :226929-39-1
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中文名称
LB42708
中文别名
LB42708 抑制剂
英文名称
LB42708
英文别名
[1-{[1-(4-Bromobenzyl)-1H-imidazol-5-yl]methyl}-4-(1-naphthyl)-1H -pyrrol-3-yl](4-morpholinyl)methanone;LB42708;4-[[1-[[1-[(4-Bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]carbonyl]morpholine;LB 42708;(1-((1-(4-Bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone;[1-[[3-[(4-bromophenyl)methyl]imidazol-4-yl]methyl]-4-naphthalen-1-ylpyrrol-3-yl]-morpholin-4-ylmethanone;(E)-N'-(2,4-dimethylphenyl)-N-((E)-((2,4-dimethylphenyl)imino)methyl)-N-methylformimidamide;C30H27BrN4O2;GTPL8029;AOB5
Cas No.
226929-39-1
分子式
C30H27BrN4O2
分子量
555.47
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
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。
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 IC 50 s of 0.8 nM, 1.2 nM and 2.0 nM, respectively.
性状
Solid
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Hee-Jun Na, et al. Inhibition of farnesyltransferase prevents collagen-induced arthritis by down-regulation of inflammatory gene expression through suppression of p21(ras)-dependent NF-kappaB activation. J Immunol. 2004 Jul 15;173(2):1276-83.
[2]. Han-Soo Kim, et al. The farnesyltransferase inhibitor, LB42708, inhibits growth and induces apoptosis irreversibly in H-ras and K-ras-transformed rat intestinal epithelial cells. Toxicol Appl Pharmacol. 2006 Sep 15;215(3):317-29.
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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