LB42708

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LB42708 是一种口服活性法呢基转移酶 (FTase) 抑制剂（对于 H/N/K-ras，IC50：0.8/1.2/2.0 nM）。

LB42708 is a potent, orally active and selective nonpeptidic farnesyltransferase inhibitor (FTase inhibitor). LB42708 inhibited VEGF-induced Ras activation and subsequently suppressed angiogenesis in vitro and in vivo by blocking the mitogen-activated protein kinase kinase/extracellular signal-regulated kinase/p38 mitogen-activated protein kinase (MAPK) and phosphatidylinositol 3-kinase (PI3K)/Akt/endothelial nitric-oxide synthase pathways in endothelial cells without altering FAK/Src activation.

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.

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LB42708 | LB-42708 | LB 42708

Others

Other Targets

Farnesyl transferase (FTase)| Farnesyl transferase (FTase)| Farnesyl transferase (FTase)

Cancer

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226929-39-1

555.46

C30H27BrN4O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (180.03 mM)

Brc1ccc(Cn2cncc2Cn2cc(C(=O)N3CCOCC3)c(c2)c2cccc3ccccc23)cc1

(1-((1-(4-bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone

(-20℃)

With Ice Pack

≥ 2 years