| Bioactivity | OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC50 of 5 μM[1][3]. | ||||||||||||
| Target | IC50: 5 μM (PDK-1) | ||||||||||||
| Invitro | OSU-03012 抑制 PC-3 细胞活力，IC50 值为 5 μM。研究了 OSU-03012 在添加 10% FBS 的培养基中对 PC-3 细胞增殖的影响。OSU-03012 在 1% FBS 的培养基中诱导 PC-3 细胞凋亡，呈剂量依赖性。该过程导致了 DNA 断裂和 PARP 切割。OSU-03012 能有效抑制 PC-3 细胞在亚 μM 水平的增殖，与 1% 血清的结果一致[1]。 | ||||||||||||
| In Vivo | 所有 SCID/Rag2 小鼠均出现 2 个 MDA-MB-435/LCC6/Her-2 肿瘤，并被分配到对照或 OSU-03012 (200 mg/kg) 治疗组，口服 3 天。与接受载体对照的小鼠肿瘤相比，OSU-03012 显著降低肿瘤中 EGFR 蛋白的表达水平约 48%。OSU-03012还能阻止 Y-box 结合蛋白-1 (YB-1) 在 1b 和 2a 位点与 EGFR 启动子结合[2]。 | ||||||||||||
| Name | OSU-03012 | ||||||||||||
| CAS | 742112-33-0 | ||||||||||||
| Formula | C26H19F3N4O | ||||||||||||
| Molar Mass | 460.45 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Zhu J, et al. From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors. Cancer Res. 2004 Jun 15;64(12):4309-18. [2]. To K, et al. The phosphoinositide-dependent kinase-1 inhibitor 2-amino-N-[4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-acetamide (OSU-03012) prevents Y-box binding protein-1 from inducing epidermal growth factor receptor. Mol Pharmacol. 2007 Sep;72(3):641-52. [3]. Tina X Lee, et al.Growth Inhibitory and Anti-Tumour Activities of OSU-03012, a Novel PDK-1 Inhibitor, on Vestibular Schwannoma and Malignant Schwannoma Cells. Eur J Cancer |