產(chǎn)品屬性:
產(chǎn)品名稱
規(guī)格
CAS號
型號
L-778123 hydrochloride (L-778,123 hydrochloride)
10mM*1mLinDMSO 5mg 10mg 50mg 100mg
253863-00-2
EY-Y0164389
Cas No.253863-00-2
別名 N/A
化學(xué)名 N/A
分子式 C22H21Cl2N5O
分子量 442.34
溶解度 DMSO : ≥ 25 mg/mL (56.52 mM)
儲存條件 Store at -20°C General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. Shipping Condition Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request 產(chǎn)品描述: L-778123 hydrochloride is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.IC50 value: 2 nM [1]Target: FPTasein vitro: L-778123 can completely inhibit Ki-Ras prenylation. [1] L-778123 as a farnesyltransferase inhibitor can have a good cytotoxic activity as a classic anti-cancer agent. [2]in vivo: In the dog model, L-778123 inhibits HDJ2 prenylation and produces measurable, albeit slight (5%), levels of unprenylatedRap1A in PBMCs. [1]
[1]. Lobell RB, et al. Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I. Mol Cancer Ther. 2002 Jul;1(9):747-758. [2]. Ghasemi S, et al. Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines. Adv Pharm Bull. 2013;3(1):73-77.
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