Home Metabolism FTase inhibitor - Transferase inhibitor LB42708 For research use only.

LB42708

LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively.

LB42708 Chemical Structure

LB42708 Chemical Structure

CAS No. 226929-39-1

Purity & Quality Control

Batch: S746701 DMSO]100 mg/mL]false]Ethanol]86 mg/mL]false]Water]Insoluble]false Purity: 100.0%
100.0

LB42708 Related Products

Biological Activity

Description LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively.
Targets
FTase (H-ras) [1] FTase (N-ras) [1] FTase (K-Ras) [1]
0.8 nM 1.2 nM 2.0 nM
In vitro
In vitro LB42708 potently inhibits the processing of the cellular farnesylated protein p21ras induced by LPS + IFN-γ in murine macrophage cell line RAW264.7 cells. LB42708 inhibits NF-κB activation and iNOS promoter activity through the inhibition of IKK activity. Moreover, LB42708 suppresses the expression of inducible NO synthase, cyclooxygenase-2, TNF-alpha, and IL-1beta and the production of NO and PGE(2) in immune-activated macrophages and osteoblasts. [1] LB42708 irreversibly inhibits growth and induces apoptosis in H-ras and K-ras-transformed rat intestinal epithelial cells. [2] LB42708 inhibits of VEGF-induced tumor angiogenesis by blocking Ras-dependent MAPK and PI3K/Akt pathways in tumor-associated endothelial cells. [3]
Cell Research Cell lines RIE-1 cells stably transformed with either activated H-ras (RIE/H-ras) or K-ras4B (RIE/K-ras).
Concentrations ~25 μM
Incubation Time 72 hours
Method

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.
In Vivo
In 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. [1] LB42708 (20 mg/kg/day i.p.) also inhibits tumor growth and angiogenesis in both Ras wild-type and mutated tumors. [3]
Animal Research Animal Models Mice collagen-induced arthritis model.
Dosages 10 mg/kg daily
Administration i.p.

Chemical Information & Solubility

Molecular Weight 555.46 Formula

C30H27BrN4O2
CAS No. 226929-39-1 SDF Download LB42708 SDF
Smiles C1COCCN1C(=O)C2=CN(C=C2C3=CC=CC4=CC=CC=C43)CC5=CN=CN5CC6=CC=C(C=C6)Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (180.03 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble


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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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