Home Tools

LB42708

Catalog No. T2678 CAS 226929-39-1

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

LB42708, CAS 226929-39-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 42.00
2 mg	In stock	$ 58.00
5 mg	In stock	$ 88.00
10 mg	In stock	$ 148.00
25 mg	In stock	$ 292.00
50 mg	In stock	$ 436.00
100 mg	In stock	$ 611.00
1 mL * 10 mM (in DMSO)	In stock	$ 135.00

Bulk Inquiry

Select Batch

Purity: 97.83%

Biological Description

Chemical Properties

Storage & Solubility Information

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 (H-ras):0.8 nM, FTase (K-Ras):2.0 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)

Molecular Weight	555.47
Formula	C30H27BrN4O2
CAS No.	226929-39-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 55.6 mg/mL (100 mM)

DMSO: 55.6 mg/mL (100 mM)

References and Literature

1. Na HJ, et al. J Immunol. 2004, 173(2), 1276-1283. 2. Kim HS, et al. Toxicol Appl Pharmacol. 2006, 215(3), 317-329. 3. Kim CK, et al. Mol Pharmacol. 2010, 78(1), 142-150

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

Sinbaglustat DGAT-1 inhibitor 2 Lonafarnib DGAT1-IN-1 Ervogastat Risedronate Sodium Entacapone acid Alendronate sodium hydrate

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

LB42708 226929-39-1 Metabolism Transferase Ftase Apoptosis Inhibitor H-Ras orally active K-Ras4B N-Ras Farnesyl Transferase inhibit LB-42708 farnesyltransferase inhibitor LB 42708 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.