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
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

LB 42708 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

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.

All Tocris products are intended for laboratory research use only.

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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Safety Datasheet

References

References are publications that support the products' biological activity.

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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Keywords: LB 42708, supplier, LB42708, ftase, farnesyltransferase, inhibitors, inhibits, selective, Protein, Prenyltransferases, Post-translational, Modifications, Protein, Prenyltransferases, Tocris Bioscience

Citations for LB 42708

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis

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