| Name | 2-morpholin-4-yl-8-phenylchromen-4-one,hydrochloride |
|---|---|
| Synonyms |
LY-294,002 hydrochloride, (HPLC)
LY 294002, Hydrochloride Salt LY-294002 hydrochloride, 10 mM in DMSO LY-294,002 hydrochloride selective inhibitor of PI 3-kinase 2-morpholino-8-phenyl-4H-chromen-4-one hydrochloride 2-Morpholin-4-yl-8-phenyl-4H-chromen-4-one HCl |
| Description | LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research[1][2][3]. |
|---|---|
| Related Catalog | |
| Target |
CK2:0.098 μM (IC50) CK2α2:3.869 μM (IC50) |
| In Vitro | LY294002 hydrochloride (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion[4]. LY294002 hydrochloride (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent[4]. LY294002 hydrochloride (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[4]. LY294002 hydrochloride (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[6]. Cell Proliferation Assay Cell Line: CNE-2Z cells[4] Concentration: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM Incubation Time: 24 hours and 48 hours Result: Decreased CNE-2Z cells in a dose-dependent fashion. Apoptosis Analysis Cell Line: CNE-2Z cells[4] Concentration: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM Incubation Time: 24 hours and 48 hours Result: Induced apoptosis rate in a dose-dependent manner. Western Blot Analysis Cell Line: CNE-2Z cells[4] Concentration: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM Incubation Time: 24 hours and 48 hours Result: Decreased phosphorylated Akt (S473) expression levels were significantly, up-regulated caspase-9 activity in CNE-2Z cells in treated group. |
| In Vivo | LY294002 hydrochloride (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[4]. LY294002 hydrochloride (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[5]. Animal Model: Athymic nude mice (6-8 weeks) with CNE-2Z xenograft[4] Dosage: 10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg Administration: IP; twice weekly, for 4 weeks Result: Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner. |
| References |
| Molecular Formula | C19H18ClNO3 |
|---|---|
| Molecular Weight | 343.80400 |
| Exact Mass | 343.09800 |
| PSA | 42.68000 |
| LogP | 4.16360 |
| Storage condition | 2-8°C |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |