LY294002
产品说明书
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同义名 : | SF 1101;NSC 697286 |
| CAS号 : | 154447-36-6 | |
| 货号 : | A133122 | |
| 分子式 : | C19H17NO3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 307.343 | |
| MDL号 : | MFCD00270881 | |
| 存储条件： |
Pure form Sealed in dry,Store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(162.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 50 mg/mL(162.68 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
5% DMSO+ 40%PEG 300+5% Tween 80+50%water 3 mg/mL |
| 生物活性 | |||
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| 靶点 |
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| 描述 | PI3Ks (Phosphatidylinositol-4,5-bisphosphate 3-kinase) participate in a diverse array of process, including the regulation of cellular survival, differentiation and stem cell-like properties, growth, proliferation, metabolism, migration, and angiogenesis[2]. LY294002 is the first synthetic molecule to inhibit p110α, p110β and p110δ, which is the 110 kDa catalytic subunit of class IA PI3Ks, with IC50 value of 0.5 μM, 0.57 μM, 0.97 μM (determined using the PI3K lipid kinase assays on recombinant protein), respectively[1]. LY294002 can induce apoptosis of human nasopharyngeal carcinoma in vitro and in vivo[3], induce a senescence-like growth arrest in human diploid fibroblasts[4], decrease invasion and migration of human ovarian carcinoma cells[5]. Also it can be used as an autophagy inhibitor[6]. | ||
| 作用机制 | LY294002 acts at the ATP-binding site of the PI3Ks enzyme.[7] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| HEK293 cells | Function assay | 1.5 h | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting | 22537153 | |
| HeLa (human carcinoma) cells. | Function assay | In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=1.4 μM. | 15658870 | ||
| HeLa cells | Function assay | Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM. | 15658870 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02337309 | Neuroblastoma | Phase 1 | Terminated(Low patient accrual... 展开 >>) 收起 << | - | United States, California ... 展开 >> Children's Hospital Los Angeles Los Angeles, California, United States, 90027-0700 UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94143 United States, Colorado Children Hospital of Colorado Aurora, Colorado, United States, 80045 United States, Georgia AFLAC Cancer Center and Blood Disorders Service of Children's Healthcare of Atlanta - Egleston Campus Atlanta, Georgia, United States, 30322 United States, Illinois University of Chicago Comer Children's Hospital Chicago, Illinois, United States, 60637 United States, Massachusetts Childrens Hospital Boston, Dana-Farber Cancer Institute. Boston, Massachusetts, United States, 02115 United States, Michigan C.S Mott Children's Hospital Ann Arbor, Michigan, United States, 48109 United States, North Carolina University of North Carolina Chapel Hill, North Carolina, United States, 27599 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229-3039 United States, Texas Cook Children's Healthcare System Fort Worth, Texas, United States, 76104 United States, Washington Children's Hospital and Regional Medical Center - Seattle Seattle, Washington, United States, 98105 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.25mL 0.65mL 0.33mL |
16.27mL 3.25mL 1.63mL |
32.54mL 6.51mL 3.25mL |
