LB42708

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WARNING: This product is for research use only, not for human or veterinary use.

Description: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.

Price and Availability

LB42708, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS docum ents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406418Name: LB42708CAS#: 226929-39-1Chemical Formula: C30H27BrN4O2Exact Mass: 554.13174Molecular Weight: 555.46Elemental Analysis: C, 64.87; H, 4.90; Br, 14.39; N, 10.09; O, 5.76

Synonym:LB42708; LB-42708; LB 42708.

IUPAC/Chemical Name:(1-((1-(4-bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone

InChi Key:GUUIRIMAQGOLHT-UHFFFAOYSA-N

InChi Code:InChI=1S/C30H27BrN4O2/c31-24-10-8-22(9-11-24)17-35-21-32-16-25(35)18-33-19-28(27-7-3-5-23-4-1-2-6-26(23)27)29(20-33)30(36)34-12-14-37-15-13-34/h1-11,16,19-21H,12-15,17-18H2

SMILES Code:O=C(C1=CN(CC2=CN=CN2CC3=CC=C(Br)C=C3)C=C1C4=C5C=CC=CC5=CC=C4)N6CCOCC6

Technical Data

Additional Information

References

1: Moorthy NS, Sousa SF, Ramos MJ, Fernandes PA.Farnesyltransferase inhibitors: a comprehensive review based onquantitative structural analysis. Curr Med Chem. 2013;20(38):4888-923.PubMed PMID: 24059235.

2: Kim CK, Choi YK, Lee H, Ha KS, Won MH, Kwon YG, Kim YM. Thefarnesyltransferase inhibitor LB42708 suppresses vascular endothelialgrowth factor-induced angiogenesis by inhibiting ras-dependent mitogen-activatedprotein kinase and phosphatidylinositol 3-kinase/Akt signal pathways.Mol Pharmacol. 2010 Jul;78(1):142-50. doi: 10.1124/mol.110.063586. Epub2010 Apr 20. PubMed PMID: 20406854.

3: Kim HS, Kim JW, Gang J, Wen J, Koh SS, Koh JS, Chung HH, Song SY. Thefarnesyltransferase inhibitor, LB42708, inhibits growth and inducesapoptosis irreversibly in H-ras and K-ras-transformed rat intestinalepithelial cells. Toxicol Appl Pharmacol. 2006 Sep 15;215(3):317-29.Epub 2006 May 19. PubMed PMID: 16712893.

4: Na HJ, Lee SJ, Kang YC, Cho YL, Nam WD, Kim PK, Ha KS, Chung HT, LeeH, Kwon YG, Koh JS, Kim YM. Inhibition of farnesyltransferase preventscollagen-induced arthritis by down-regulation of inflammatory geneexpression through suppression of p21(ras)-dependent NF-kappaBactivation. J Immunol. 2004 Jul 15;173(2):1276-83. PubMed PMID:15240720.

5: Kim KW, Chung HH, Chung CW, Kim IK, Miura M, Wang S, Zhu H, Moon KD,Rha GB, Park JH, Jo DG, Woo HN, Song YH, Kim BJ, Yuan J, Jung YK.Inactivation of farnesyltransferase and geranylgeranyltransferase I bycaspase-3: cleavage of the common alpha subunit during apoptosis.Oncogene. 2001 Jan 18;20(3):358-66. PubMed PMID: 11313965.