LB42708

Alias: LB-42708; LB 42708; LB42708;
Cat No.:V0921 Purity: ≥98%
LB42708 (LB-42708; LB 42708) is a novel, potent, orally bioactive, and nonpeptidic farnesyltransferase (FTase) inhibitor with potential anti-inflammatory activity.
LB42708 Chemical Structure CAS No.: 226929-39-1
Product category: Transferase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

LB42708 (LB-42708; LB 42708) is a novel, potent, orally bioactive, and nonpeptidic farnesyltransferase (FTase) inhibitor with potential anti-inflammatory activity. It inhibits H-ras, N-ras, and K-ras with IC50 of 0.8, 1.2, and 2.0 nM, respectively. LB42708 demonstrates significant in vivo efficacy in mice collagen-induced arthritis model.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
LB42708, in spite of K-ras prenylation, causes cell death. In H-ras-transformed RIE cells, LB42708 causes growth inhibition, which is accompanied by G1/M and G2/M cell cycle arrests, respectively. Ras-transformed rat intestinal epithelial (RIE) cells exhibit unique morphological changes and cell cycle arrest as a result of p21(CIP1/WAF1) and RhoB being upregulated above the basal level by LB42708[2].
ln Vivo
LB42708 (12.5 mg/kg i.p.) inhibits production of NO, PGE2, TNF-α, and IL-1β in LPS-injected mice, and also prevents the development of CIA. LB42708 (20 mg/kg/day i.p.) also inhibits tumor growth and angiogenesis in both Ras wild-type and mutated tumors.
Animal Protocol
Dissolved in Saline; 10 mg/kg; i.p. injection
Mice collagen-induced arthritis model.
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C30H27BRN4O2
Molecular Weight
555.46
CAS #
226929-39-1
SMILES
BrC1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])N1C([H])=NC([H])=C1C([H])([H])N1C([H])=C(C2=C([H])C([H])=C([H])C3=C([H])C([H])=C([H])C([H])=C23)C(=C1[H])C(N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])=O
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
Chemical Name
(1-((1-(4-bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone
Synonyms
LB-42708; LB 42708; LB42708;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (180.0 mM)
Water:<1 mg/mL
Ethanol: 86 mg/mL warmed (154.8 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8003 mL 9.0015 mL 18.0031 mL
5 mM 0.3601 mL 1.8003 mL 3.6006 mL
10 mM 0.1800 mL 0.9002 mL 1.8003 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • LB42708

    LB42708 inhibits VEGF-induced in vitro angiogenesis.Mol Pharmacol.2010 Jul;78(1):142-50.
  • LB42708

    LB42708 inhibits VEGF-induced angiogenesis ex vivo and in vitro.Mol Pharmacol.2010 Jul;78(1):142-50.
  • LB42708

    LB42708 regulates the VEGF-induced angiogenic signaling pathway.Mol Pharmacol.2010 Jul;78(1):142-50.
  • LB42708

    Specific knockdown of FTase and Ras inhibits VEGF-induced signal transduction and in vitro angiogenesis.Mol Pharmacol.2010 Jul;78(1):142-50.
  • LB42708

    LB42708 and Ras knockdown blocks VEGF-induced endothelial cell cycle progression by arresting cells at the G1 phase.Mol Pharmacol.2010 Jul;78(1):142-50.
  • LB42708

    LB42708 reduces tumor growth and angiogenesis in human tumor xenograft models.Mol Pharmacol.2010 Jul;78(1):142-50.
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