产品
编 号:F183097
分子式:C19H17NO3
分子量:307.34
产品类型
10mM*1mL in DMSO
572
In-stock
结构图
CAS No: 154447-36-6
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产品详情
生物活性:
LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4?μM. LY294002 is an apoptosis activator.
体内研究:
LY294002 (10, 25, 50, 75 mg/kg; i.p.; twice weekly; for 4 weeks) significantly reduces mean NPC tumor burden in a dose-dependent manner. LY294002 (10, 25 mg/kg) is less effective in decreasing tumor burden. LY294002 (1.2 mg/kg per day; i.p.; for 14 days) prevents Leptin (60 ug/kg)-induced adverse effects on spermatozoa in Sprague-Dawley rats.Animal Model:Athymic nude mice (6-8 weeks) with CNE-2Z xenograft
Dosage:10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg
Administration:Intraperitoneal injection; twice weekly, for 4 weeks
Result:Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner.
体外研究:
LY294002 (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion.LY294002 (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent.LY294002 (10-75 μM) significantly decreases p-Akt (S473) expression levels and up-regulates caspase-9 activity in CNE-2Z cells. Total Akt protein level is not difference with different concentration.LY294002 (5, 10, 100 μM; for 2 hours) treatment partially suppresses Lysophosphatidic acid (LPA)-induced (20 μM; for 4 hours) nuclear translocation of YAP, accompanied by a reduction in p-AKT levels.