LY294002

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种经典的广谱 PI3K 抑制剂，对 PI3Kα/δ/β 的 IC50 分别为 0.5/0.57/0.97 uM。

A classic, broad-spectrum PI3K inhibitor with IC50 of 0.5/0.57/0.97 uM for PI3Kα/δ/β, respectively; completely and specifically abolishes PI3K activity (IC50=1.4 uM), but does not inhibit PI4K or other lipid kinases; demonstrates growth-inhibitory and apoptosis-inducing effect in colon cancer cell lines, with decreased phosphorylated Akt Ser(473); suppresses tumor growth in mouse xenografts; also is a potent inhibitor of CK2 with IC50 of 98 nM.(In Vitro):LY294002 (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion.LY294002 (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent.LY294002 (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.LY294002 (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. (In Vivo):LY294002 (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.LY294002 (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.

LY294002 (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion.LY294002 (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent.LY294002 (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.LY294002 (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. Cell Proliferation Assay Cell Line:CNE-2Z cells 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 Concentration:0 μM, 10 μM, 25 μM, 50 μM, and 75 μM Incubation Time:24 hours and 48 hours Result:Induced apoptosis rate in dose-dependent. Western Blot Analysis Cell Line:CNE-2Z cells Concentration:10 μM, 25 μM, 50 μM, and 75 μM Incubation Time:Result:Decreased phosphorylated Akt (S473) expression levels were significantly, up-regulated caspase-9 activity in CNE-2Z cells in treated group.

LY294002 (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. LY294002 (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. Animal Model:Athymic nude mice (6-8 weeks) with CNE-2Z xenograft Dosage:10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg Administration:Intraperitoneal injection; twice weekly, for 4 weeks Result:Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner.

NSC 697286 | SF 1101 | LY 294002 | LY-294002

PI3K/Akt/mTOR signaling

PI3K

p110α|p110β|p110δ|DNA-PK

Cancer

——

154447-36-6

307.3432

C19H17NO3

>98% (HPLC)

DMSO: 14.9 mg/mL

O=C1C=C(N2CCOCC2)OC3=C(C4=CC=CC=C4)C=CC=C13

4H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl-

(-20℃)

With Ice Pack

≥ 2 years