CAS:154447-36-6LY294002

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Synonyms: SF 1101;NSC-697286

LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

154447-36-6

储存条件

分子式

C19H17NO3

运输

蓝冰

分子量

307.34

别名

SF 1101;NSC-697286

溶解度

DMSO	51.67 mg/mL (168.1 mM)
Water	insoluble

动物实验配方

5% DMSO+ 40%PEG 300+5% Tween 80+50%water

3 mg/mL

生物活性

靶点 PI3Kα

IC50:0.5μM PI3Kβ

IC50:0.97μM PI3Kδ

IC50:0.57μM
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]
动物研究
剂量
Mice: 0 - 100 mg/kg^[1] Rats: min = 50 mg/kg^[2], max = 100 mg/kg^[3]

给药途径
i.p.

动物研究
剂量	Mice: 0 - 100 mg/kg^[1] Rats: min = 50 mg/kg^[2], max = 100 mg/kg^[3]
给药途径	i.p.