<Suppliers Price>

LB 42708

Names

[ CAS No. ]:
226929-39-1

[ Name ]:
LB 42708

[Synonym ]:
[1-{[1-(4-Bromobenzyl)-1H-imidazol-5-yl]methyl}-4-(1-naphthyl)-1H-pyrrol-3-yl](4-morpholinyl)methanone
Methanone, [1-[[1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinyl-
LB42708

Biological Activity

[Description]:

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[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Metabolic Enzyme/Protease >> Farnesyl Transferase

[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[2].

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
769.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C30H27BrN4O2

[ Molecular Weight ]:
555.465

[ Flash Point ]:
419.2±32.9 °C

[ Exact Mass ]:
554.131714

[ PSA ]:
52.29000

[ LogP ]:
3.14

[ Vapour Pressure ]:
0.0±2.6 mmHg at 25°C

[ Index of Refraction ]:
1.681

[ Storage condition ]:
-20℃

Related Compounds