LB 42708

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Cat.No. 4294 - LB 42708 | C30H27BrN4O2 | CAS No. 226929-39-1
Description: Selective farnesyltransferase (FTase) inhibitor
Chemical Name: [1-[[1-[(4-Bromophenyl)methyl]-1H-imidazol-5-yl]methyl]-4-(1-naphthalenyl)-1H-pyrrol-3-yl]-4-morpholinylmethanone
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Selective inhibitor of farnesyltransferase (FTase). Blocks farnesylation of H-Ras, N-Ras and K-Ras4B (IC50 values are 0.8, 1.2 and 2.0 nM respectively). Displays >50,000-fold selectivity for FTase over geranylgeranyltransferase (GGTase) I. Inhibits VEGF-induced Ras activation; suppresses angiogenesis in vivo and in vitro (IC50 = 75 nM). Orally active.

Compound Libraries

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Technical Data

M. Wt 555.46
Formula C30H27BrN4O2
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 226929-39-1
PubChem ID 10099206
InChI Key GUUIRIMAQGOLHT-UHFFFAOYSA-N
Smiles O=C(N4CCOCC4)C1=CN(CC5=CN=CN5CC6=CC=C(Br)C=C6)C=C1C2=CC=CC3=C2C=CC=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.55 100
ethanol 55.55 100

Preparing Stock Solutions

The following data is based on the product molecular weight 555.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.8 mL 9 mL 18 mL
5 mM 0.36 mL 1.8 mL 3.6 mL
10 mM 0.18 mL 0.9 mL 1.8 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Na et al (2004) Inhibition of farnesyltransferase prevents collagen-induced arthritis by down-regulation of inflammatory gene expression through suppresion of p21ras-dependent NF-κB activation. J.Immunol. 173 1276 PMID: 15240720

Kim et al (2010) The farnesyltransferase inhibitor LB42708 suppresses vascular endothelial growth factor-induced angiogenesis by inhibiting Ras-dependent mitogen-activated protein kinase and phosphatidylinositol 3-kinase/Akt signal pathways. Mol.Pharmacol. 78 142 PMID: 20406854


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Citations for LB 42708

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