LB42708

Catalog No.S7467 Batch:S746701

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Technical Data

Formula

C30H27BrN4O2
Molecular Weight 555.46 CAS No. 226929-39-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (180.03 mM)
Ethanol 86 mg/mL (154.82 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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]
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]

Protocol (from reference)

Cell Assay:

[2]
  • 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.
Animal Study:

[1]
  • Animal Models

    Mice collagen-induced arthritis model.

  • Dosages

    10 mg/kg daily

  • Administration

    i.p.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.