產(chǎn)品目錄

規(guī)格	5mg 10mg 25mg 100mg
CAS	603288-22-8
別名	LY 2090314;LY-2090314
化學(xué)名	3-(9-fluoro-2-(piperidine-1-carbonyl)-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl)-4-(imidazo[1,2-a]pyridin-3-yl)-1H-pyrrole-2,5-dione
分子式	C28H25FN6O3
分子量	512.53
溶解度	≥ 91 mg/mL in DMSO, ≥ 4.27 mg/mL in EtOH with ultrasonic and warming
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：

IC50: 1.5 nM (GSK-3α); 0.9 nM (GSK-3β)

LY2090314 (LY) is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in various pathways, such as protein synthesis initiation, cell proliferation/differentiation, and apoptosis.

In vitro: LY2090314 selectively inhibits the activity of GSK-3 by inhibiting ATP binding. LY2090314 was reported to be able to stabilize β-catenin. As monotherapy, LY2090314 aslso showed limited efficacy. In solid tumor cancer cell lines, LY3090314 was found to enhance the efficacy of cisplatin and carboplatin [1].

In vivo: Even in Mdr1a-, Bcrp-, and Mrp2-knockout rats, the metabolites of LY2090314 did not appear in systemic circulation, and the urinary excretion was not found to be enhanced, since the hypothesized impaired biliary excretion of metabolites in the absence of these canalicular transporters was not observed. Dog metabolite disposition was similar, with the exception of LY2090314 glucuronide. Moreover, LY2090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts [1]

Clinical trial: In advanced solid tumor patients (pts), LY2090314 (LY) was dosed intravenously as a lead-in 7 days prior to the first administration of the triplet combination with PC. Preliminary pharmacokinetic analyses showed that exposure increased as dose increased over the dose range studied with a short terminal elimination half-life calculated in the majority of patients. Large number of pretreated patients that experienced stable disease suggests continued evaluation of LY in NSCLC may be warranted.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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