| Description | LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation. |
| In vitro | LY294002通过失活Akt/PKB，从而抑制细胞增殖并诱导凋亡。在这些结肠癌细胞系中，LY294002表现出显著的生长抑制和诱导凋亡效应，并降低磷酸化Akt（Ser473）[2]的表达。LY294002使肿瘤细胞的胞质体积减小，核固缩明显。此外，LY294002还特异性引起细胞生长G1期阻滞，几乎完全抑制黑色素瘤细胞的增殖，并部分抑制MG-63（成骨肉瘤细胞系）的增殖[3]。 |
| In vivo | LY294002能有效抑制肿瘤生长并诱导凋亡，特别是在LoVo肿瘤中表现出显著效果。因此，在小鼠腹膜炎癌症模型中展现出了卓越的效能[2]。LY294002显著地抑制卵巢癌的生长和腹水形成[3]。 |
| Cell experiments | Cell lines: Colon cancer cell lines DLD-1,LoVo,HCT15,and Colo205. Concentrations: 0–50 μM. Incubation Time: 0–48 hours. Method: 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,Premix WST-1 (10 μL) is 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.[2] |
| Animal experiments | 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. Dosages: 0–100 mg/kg. Administration: i.p.[3] |
| Target activity | PI3Kα:0.5μM, PI3Kβ:0.97 μM, PI3Kδ:0.57μM |
| Synonyms | SF 1101, LY 294002, NSC 697286 |
| molecular weight | 343.81 |
| Molecular formula | C19H17NO3·HCl |
| CAS | 934389-88-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (145.43 mM) Ethanol: 5 mM |
| References | 1. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. 2. Semba S, et al. The in vitro and in vivo effects of 2-(4-morpholinyl)-8-phenyl-chromone (LY2942002), a specific inhibitor of phosphatidylinositol 3'-kinase, in human colon cancer cells. Clin Cancer Res. 2002 Jun;8(6):1957-63. 3. Hu L, et al. In vivo and in vitro ovarian carcinoma growth inhibition by a phosphatidylinositol 3-kinase inhibitor (LY2942002). Clin Cancer Res. 2000 Mar;6(3):880-6. 4. Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY2942002. Biochem J. 2007 May 15;404(1):15-21. |