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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
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.
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].
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ln Vivo |
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Animal Protocol |
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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. |
Molecular Formula |
C30H27BRN4O2
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Molecular Weight |
555.46
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CAS # |
226929-39-1
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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
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InChi Key |
GUUIRIMAQGOLHT-UHFFFAOYSA-N
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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
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Chemical Name |
(1-((1-(4-bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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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.
Calculation results
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.
(2) Be sure to add the solvent(s) in order.