LB 42708
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- Product name: LB 42708
- CAS: 226929-39-1
- MF: C30H27BrN4O2
- MW: 555.47
- EINECS:
- MDL Number:MFCD20926350
- Synonyms:LB 42708;[1-[[1-[(4-Bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinylmethanone;[1-[[1-[(4-Bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinylmethanone LB42708;4-[[1-[[1-[(4-Bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]carbonyl]morpholine;[1-{[1-(4-bromobenzyl)-1h-imidazol-5-yl]methyl}-4-(1-naphthyl)-1h -pyrrol-3-yl](4-morpholinyl)methanone;LB-42708;LB 42708;CS-1450;Methanone, [1-[[1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinyl-
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Properties
Boiling point :769.6±60.0 °C(Predicted)
Density :1.39±0.1 g/cm3(Predicted)
storage temp. :Store at -20°C
solubility :≥22.75 mg/mL in DMSO; insoluble in H2O; ≥47.5 mg/mL in EtOH
pka :5.67±0.13(Predicted)
form :solid
color :Off-white to light yellow
Density :1.39±0.1 g/cm3(Predicted)
storage temp. :Store at -20°C
solubility :≥22.75 mg/mL in DMSO; insoluble in H2O; ≥47.5 mg/mL in EtOH
pka :5.67±0.13(Predicted)
form :solid
color :Off-white to light yellow
Safety Information
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Description
Farnesylation, the post-translational addition of a 15-carbon isoprenyl group, alters the function of several proteins, including Ras proteins. LB 42708 is a potent inhibitor of farnesyltransferase (FTase), blocking farnesylation of H-Ras, N-Ras, and K-Ras4B with IC50 values of 0.8, 1.2, and 2.0 nM, respectively. It displays over 50,000-fold selectivity for FTase over geranylgeranyltransferase I. LB 42708 prevents the farnesylation of H-Ras in response to LPS plus IFN-γ (IC50 = 10 nM), preventing activation of NF-κB as well as downstream signaling. These effects are obtained both in RAW 264.7 mouse macrophages and in mice. LB42708 also inhibits Ras-dependent signaling in endothelial cells, stopping VEGF-mediated angiogenesis both in vitro and in vivo.Related product price
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