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LB42708

🥰Excellent
Catalog No. T2678Cas No. 226929-39-1

LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).

LB42708

LB42708

🥰Excellent
Purity: 97.83%
Catalog No. T2678Cas No. 226929-39-1
LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).
Pack SizePriceAvailabilityQuantity
1 mg$42In Stock
2 mg$58In Stock
5 mg$88In Stock
10 mg$148In Stock
25 mg$292In Stock
50 mg$436In Stock
100 mg$611In Stock
1 mL x 10 mM (in DMSO)$135In Stock
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Purity:97.83%
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Product Introduction

Bioactivity
Description
LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).
Targets&IC50
FTase (K-Ras):2.0 nM, FTase (H-ras):0.8 nM, FTase (N-ras):1.2 nM
In vitro
In mice treated with lipopolysaccharide (LPS), LB42708 (12.5 mg/kg, intraperitoneally) inhibited the production of nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-α), and interleukin-1 beta (IL-1β), and suppressed the progression of collagen-induced arthritis (CIA). Additionally, in tumors with either wild-type or mutated Ras, LB42708 (20 mg/kg/day, intraperitoneally) inhibited tumor growth and angiogenesis.
In vivo
LB42708 exerts an irreversible inhibitory effect on growth and induces apoptosis in rat intestinal epithelial cells altered by H-ras and K-ras. It inhibits VEGF-induced tumor angiogenesis in tumor-associated endothelial cells by blocking the Ras-dependent MAPK and PI3K/Akt signaling pathways. Additionally, in the murine macrophage lineage RAW264.7 cells, LB42708 significantly inhibits the process of lipopolysaccharide + IFN-γ induced intracellular farnesylation of the protein p21ras. In immune-activated osteoblasts and macrophages, LB42708 suppresses the production of nitric oxide synthase, cyclooxygenase-2, TNF-α, IL-1β, NO, and PGE(2). By inhibiting IKK activity, LB42708 also represses the activation of NF-κB and the activity of the iNOS promoter.
Kinase Assay
Biochemical Assessment of PDGFRα Kinase Activity: Chinese hamster ovary (CHO) cells are transiently transfected with mutated or wild type PDGFRα constructs and treated with various concentrations of Crenolanib. Experiments involving recombinant DNA are performed using biosafety level 2 conditions in accordance with guidelines. Protein lysates from cell lines are prepared and subjected to immunoprecipitation using anti-PDGFRα antibodies followed by sequential immunoblotting for PDGFRα. Densitometry is performed to quantify drug effect using Photoshop software, with the level of phosphor- PDGFRα normalized to total protein. Densitometry and proliferation experimental results are analyzed using Calcusyn 2.1 software to mathematically determine the IC50 values. The Wilcoxon Rank Sum Test is used to compare the IC50 values of Crenolanib for a given mutation.
Cell Research
Cell growth is measured by MTT. Briefly, cells were seeded at 2 × 103 cells per well in 96-well culture plates in triplicate. After the addition of various concentrations of drugs, cells are incubated for 72 h. At the end of culture, the plates are washed twice with PBS, and cells are incubated with 200 μl of RPMI 1640 containing 10% FCS and 0.25 mg/ml of MTT at 37 °C for 3 h. The absorbance of each well is measured with Titer-Tech 96-well multiscanner at 570 nm. The viable cell number is proportional to the absorbance. (Only for Reference)
Chemical Properties
Molecular Weight555.47
FormulaC30H27BrN4O2
Cas No.226929-39-1
SmilesC(=O)(C=1C(=CN(CC=2N(CC3=CC=C(Br)C=C3)C=NC2)C1)C=4C5=C(C=CC4)C=CC=C5)N6CCOCC6
Relative Density.1.39 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 55.6 mg/mL (100 mM)
DMSO: 45 mg/mL (81.01 mM), Sonication is recommended.
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM1.8003 mL9.0014 mL18.0028 mL90.0139 mL
5 mM0.3601 mL1.8003 mL3.6006 mL18.0028 mL
10 mM0.1800 mL0.9001 mL1.8003 mL9.0014 mL
20 mM0.0900 mL0.4501 mL0.9001 mL4.5007 mL
50 mM0.0360 mL0.1800 mL0.3601 mL1.8003 mL
Ethanol
1mg5mg10mg50mg
100 mM0.0180 mL0.0900 mL0.1800 mL0.9001 mL

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