LY294002-NSC-697286-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELY294002Cat. No.: HY-10108CAS No.: 154447-36-6Synonyms: NSC 697286; SF 1101分式: CHNO分量: 307.34作靶点: PI3K; Autophagy作通路: PI3K/Akt/mTOR; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO :

2、 14.9 mg/mL (48.48 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.2537 mL 16.2686 mL 32.5373 mL5 mM 0.6507 mL 3.2537 mL 6.5075 mL10 mM 0.3254 mL 1.6269 mL 3.2537 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验

3、结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.13 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.13 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% c

4、orn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (8.13 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 LY294002种谱 PI3K 抑制剂，抑制 PI3K, PI3K 和 PI3K的 IC50 分别为 0.5, 0.57, 0.97 M 1。LY294002 也可抑制 CK2 的活性，IC50 为 98 nM 2。IC50 & Target p110 p110 p110 human CK20.5 M (IC50) 0.57 M (IC50) 0

5、.97 M (IC50) 98 nM (IC50)human CK22 Autophagy3.869 M (IC50)体外研究LY294002 (0-75 M; 24 hours and 48 hours) remarkably decreases CNE-2Z cells in a dose-dependentfashion 3.LY294002 (0-75 M; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent 3.LY294002 (10-75 M) significantly de

6、creases p-Akt (S473) expression levels and up-regulates caspase-9activity in CNE-2Z cells. Total Akt protein level is not difference with different concentration 3.Cell Proliferation Assay 3Cell Line: CNE-2Z cellsConcentration: 0 M, 10 M, 25 M, 50 M, and 75 MIncubation Time: 24 hours and 48 hoursRes

7、ult: Decreased CNE-2Z cells in a dose-dependent fashion.Apoptosis Analysis 3Cell Line: CNE-2Z cellsConcentration: 0 M, 10 M, 25 M, 50 M, and 75 MIncubation Time: 24 hours and 48 hoursResult: Induced apoptosis rate in dose-dependent.Western Blot Analysis 3Cell Line: CNE-2Z cellsConcentration: 10 M, 2

8、5 M, 50 M, and 75 MIncubation Time:Result: Decreased phosphorylated Akt (S473) expression levels were significantly, up-regulated2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEcaspase-9 activity in CNE-2Z cells in treated group.体内研究 Treatment with LY294002 (i.p.,50 mg/kg, 75 mg/kg) significantly r

9、educes mean NPC tumor burden ascompared with the control group. Treatment with 10 mg/kg or 25 mg/kg LY294002 is less effective indecreasing tumor burden. Mean NPC tumor burden treated with LY294002 is remarkably decreased in adose-dependent manner, whereas mean body weight is no obvious difference b

10、etween control and treatedgroups (LY294002, 10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg) 3.Animal Model: Athymic nude mice (6-8 weeks) with CNE-2Z xenograft 3Dosage: 10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kgAdministration: Intraperitoneal injection; twice weekly, for 4 weeksResult: Mean Nasopharynge

11、al carcinoma (NPC) tumor burden was remarkably decreased in adose-dependent manner, whereas mean body weight was no obvious differencebetween control and treated groups.户使本产品发表的科研献 Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Blood. 2018 Jul 12;132(2):210-222. J Pineal Res. 2019 Apr;66(3):e12

12、552. Nat Commun. 2019 Jan 28;10(1):453. J Exp Med. 2016 Dec 12;213(13):2989-3005.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms. Biochem J. 2007 Jun 15;404(3):449-58.2. Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21.3. Jiang H, et al. Phosphatidylinositol 3-kinase inhibitor(LY294002) induces apoptosis of human nasopharyngeal carcinoma invitro and invivo. J Exp Clin Cancer Res. 2010 Apr 22;29:34.McePdfHe