WAY-600 _mTOR 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEWAY-600Cat. No.: HY-15272CAS No.: 1062159-35-6分式: CHNO分量: 494.59作靶點(diǎn): mTOR作通路: PI3K/Akt/mTOR儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (101.09 mM; Need ultrasonic)H2O : 40% PEG

2、300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.05 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.05 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 WAY-600是有效，ATP 競(jìng)爭(zhēng)型，選擇性的 mTOR 抑制劑，抑制重 組 mTOR 酶的 IC50 值為 9 nM。WAY-600 阻斷 mT

3、OR 復(fù)合物 1/2 (mTORC1/2) 組裝和激活。IC50 & Target mTOR mTORC1 mTORC2 PI3K alpha9 nM (IC50) 1.96 M (IC50)PI3K gamma8.45 M (IC50)體外研究 WAY-600 exhibits a concentration-dependent and time-dependent inhibition of f HepG2 and Huh-7 cellsviability. Following WAY-600 (1-1000 nM) treatment, the number of HepG2 cell

4、colonies is dramaticallydecreased. Meanwhile, BrdU incorporation in HepG2 cells is also inhibited with WAY-600 treatment. WAY-600 dose-dependently increases the activity of caspase-3 and caspase-9 in HepG2 cells. WAY-600 disruptsassemble of mTORC1 (mTOR-Raptor association) and mTORC2 (mTOR-Rictor as

5、sociation). Activation ofmTORC1 (indicated by p-S6K1 and p-4E-BP1) and mTORC2 is almost blocked by WAY-600 (100 nM) 2.體內(nèi)研究 Administration of WAY-600 (10 mg/kg, daily) inhibits HepG2 tumor growth in nude mice. Daily HepG2 tumorgrowth of WAY-600-administrated mice is significantly lower than that of v

6、ehicle control mice. Importantly, thein vivo anti-cancer activity by WAY-600 is further potentiated with the co-administration of MEK-162 (2.5mg/kg, p.o. daily) 2.PROTOCOLCell Assay 2 Established HCC cells (HepG2 and Huh-7), primary HCC cells (Pnt-1/-2/-3/-4), or THLE-2 liver cells arecultured in WA

7、Y-600 (1-1000 nM)-containing medium for 24, 48, 72, 96 hours, cell viability is tested by MTTassay 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Mice tumor xenografts are randomly divided into four groups (10 mice per group): vehicle (A

8、dministration 2 intraperitoneal or i.p.), WAY-600 (10 mg/kg, i.p. injection), MEK-162 (2.5 mg/kg, oral gavage) or WAY-600plus MEK-162 combination. The mice are monitored for activity and physical condition on daily basis, andmice body weights and tumor mass are measured weekly 2.MCE has not independ

9、ently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Biochem Biophys Res Commun. 2015 Oct 23;466(3):547-53.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Yu K, et al. Biochemical, cellular, and

10、in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target ofrapamycin. Cancer Res. 2009 Aug 1;69(15):6232-40.2. Wang K, et al. MEK-ERK inhibition potentiates WAY-600-induced anti-cancer efficiency in preclinical hepatocellular carcinoma (HCC)models. Biochem Biophys Res Commun. 2016 May 27;474(2):330-7.McePdfHeightCaution: Product has not been fully va