1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPI-3065Cat. No.: HY-12235CAS No.: 955977-50-1分式: CHFNOS分量: 506.64作靶點(diǎn): PI3K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 : 25 mg/mL (49.34 mM; Need ultrasonic)H2O : 40% PEG

2、300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.93 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.93 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 PI-3065種有效的 PI3K p110 抑制劑，IC50 和 Ki 值分別為 5 nM 和 1.5 nM；對(duì) p110，p110，p110 的

3、作較弱，IC50 分別為 910，600，10000 nM。IC50 & Target p110 p110 p1105 nM (IC50) 600 nM (IC50) 910 nM (IC50)體外研究 PI-3065 exhibits no inhibition of the growth of 4T1 cells, which do not express detectable levels of p110 1.體內(nèi)研究 PI-3065 (75 mg/kg, p.o.) inhibits the growth of 4T1 tumours in the BALB/c mice withou

4、t obvious body weightloss 1.PROTOCOLAnimal Female WT BALB/c mice are orthotopically inoculated in the mammary fat pad on day 0 with 1105 4T1Administration 1 cells. Drug (75 mg/kg PI-3065, once daily) or vehicle (0.5% methylcellulose with 0.2% Tween 80) isadministered by oral gavage from day -1 (admi

5、nistered 12 h prior to tumour cell inoculation). Tumour growthis monitored weekly by caliper measurement or by measuring luminescence using a Xenogen imagingplatform. On day 35, mice are euthanized, tumours and peripheral organs extracted for in vitro luminescencemeasurement, followed by fixation in

6、 4% PFA and H&E staining. KPC mice are allowed to develop advancedlesions of 5-10 mm (determined by ultrasound imaging) before treatment with vehicle or PI-3065 for a total of14 days.MCE has not independently 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) Cell Signa

7、l. 2016 Mar;28(3):148-56.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Ali K, et al. Inactivation of PI(3)K p110 breaks regulatory T-cell-mediated immune tolerance to cancer. Nature. 2014 Jun19;509(7505):407-11.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use