LB42708

製品コードS7467 バッチS746701

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C30H27BrN4O2
分子量 555.46 CAS No. 226929-39-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (180.03 mM)
Ethanol 86 mg/mL warmed with 50ºC water bath (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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 RIE-1 cells stably transformed with either activated H-ras (RIE/H-ras) or K-ras4B (RIE/K-ras).
濃度 ~25 μM
反応時間 72 hours
実験の流れ

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.
動物実験 動物モデル Mice collagen-induced arthritis model.
投薬量 10 mg/kg daily
投与方法 i.p.

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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