您当前所在的位置:首页 > 产品中心 > 产品信息
LY294002_分子结构_CAS_154447-36-6)
点击图片或这里关闭

LY294002

产品号 S1105 公司名称 Selleck Chemicals
CAS号 154447-36-6 公司网站 http://www.selleckchem.com
分子式 C19H17NO3 电 话 (877) 796-6397
分子量 307.34318 传 真 (832) 582-8590
纯 度 电子邮件 sales@selleckchem.com
保 存 -20°C Chembase数据库ID: 2382

产品价格信息

请登录

产品别名

标题
LY294002
IUPAC标准名
2-(morpholin-4-yl)-8-phenyl-4H-chromen-4-one
IUPAC传统名
2-(morpholin-4-yl)-8-phenylchromen-4-one

产品登记号

CAS号 154447-36-6

产品性质

作用靶点 PI3K
成盐信息 Free Base
溶解度 DMSO
保存条件 -20°C

产品详细信息

详细说明 (English)
Research Area
Description Cancer
Biological Activity
Description LY294002 is a PI3K inhibitor for p110α, p110δ and p110β with IC50 of 0.5 μM, 0.57 μM and 0.97 μM, respectively.
Targets p110α p110δ p110β
IC50 0.5 μM 0.57 μM 0.97 μM[1]
In Vitro LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]
In Vivo LY294002 also resultes in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model. [2] LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. [3]
Clinical Trials LY294002 is currently in Phase I clinical trials in patients with cancers.
Features
Protocol
Kinase Assay [4]
kinase assays PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1?μM ATP. The kinase reaction is carried out for 1?hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10?μM ATP.
Cell Assay [2]
Cell Lines Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
Concentrations 0–50 μM
Incubation Time 0–48 hours
Methods 1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates. LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours. After treatment, 10 μL of Premix WST-1 are added to each microculture well, and the plates are incubated for 60 minutes at 37oC, after which absorbance at 450 nm is measured with a microplate reader.
Animal Study [3]
Animal Models Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
Formulation Dissolved in DMSO plus 0.25 ml of PBS
Doses 0–100 mg/kg
Administration Administered via i.p.
References
[1] Chaussade C, et al. Biochem J, 2007, 404(3), 449-58.
[2] Semba S, et al. Clin Cancer Res, 2002, 8(6), 1957-63.
[3] Hu L, et al. Clin Cancer Res, 2000, 6(3), 880-6.
[4] Gharbi SI, et al. Biochem J, 2007, 404(1), 15-21.