- Radicicol
- PDK1 inhibitor
- GSK2334470
- BX-912
| OSU-03012 (AR-12)Potent PDK1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
- View current batch:
- Purity = 99.69%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
| Description | OSU-03012 is potent inhibitor of recombinant PDK-1 with IC50 value of 5 μM. | |||||
| Targets | recombinant PDK-1 | |||||
| IC50 | 5 μM | |||||
| Cell experiment [1]: | |
Cell lines | PC-3 (p53-/-) human androgen-nonresponsive prostate cancer cells |
Preparation method | The solubility of this compound in DMSO is >23mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 1, 2.5, 5, 7.5, 10 μM; 6 h |
Applications | In PC-3 (p53-/-) human androgen-nonresponsive prostate cancer cells, OSU-03012 reduced the activity of immunoprecipitated p70S6K in a dose-dependent way. OSU-03012 at sub-μM was effective in suppressing PC-3 cell proliferation. |
| Animal experiment [2]: | |
Animal models | nude mice bearing established s.c. Huh7 tumor xenografts |
Dosage form | 100 and 200 mg/kg for 28 days; gavaged |
Application | In nude mice bearing established s.c. Huh7 tumor xenografts, OSU-03012 (100 and 200 mg/kg for 28 days) inhibited Huh7 tumor growth by 39.52% and 57.59%, respectively. Compared with vehicle-treated control, OSU-03012 significantly reduced tumor volumes. OSU-03012 induced autophagy in xenograft. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Zhu J1, Huang JW, Tseng PH, Yang YT, Fowble J, Shiau CW, Shaw YJ, Kulp SK, Chen CS.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] Lee TX1, Packer MD, Huang J, Akhmametyeva EM, Kulp SK, Chen CS, Giovannini M, Jacob A, Welling DB, Chang LS.Growth inhibitory and anti-tumour activities of OSU-03012, a novel PDK-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells. Eur J Cancer. 2009 Jun;45(9):1709-20. | |
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| Cas No. | 742112-33-0 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 2-amino-N-[4-[5-phenanthren-2-yl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]acetamide | ||
| Canonical SMILES | C1=CC=C2C(=C1)C=CC3=C2C=CC(=C3)C4=CC(=NN4C5=CC=C(C=C5)NC(=O)CN)C(F)(F)F | ||
| Formula | C26H19F3N4O | M.Wt | 460.45 |
| Solubility | ≥23mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
OSU-03012 (AR-12) is an inhibitor of 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 value of 5μm, which shows 2-fold higher potency over OSU-02067 [1].
OSU-03012 has represented to suppress PC-3 cell proliferation and induce apoptosis in PC-3 cells. Expression of the constitutively active forms of PDK-1 and Akt has revealed to reduce OSU-03012-induced apoptosis in PC-3 cell [1].
OSU-03012 could potently inhibit the growth of primary human VS cells and malignant schwannoma HMS-97 cells in a dose-dependent manner. In contrast, normal human Schwann cells showed to be more resistant to OSU-03012. Additionally, OSU-03012 revealed to inhibit phosphorylation of AKT at the threonine-308 site in both VS cells and HMS-97 cells [2].
References:[1] Zhu J1, Huang JW, Tseng PH, Yang YT, Fowble J, Shiau CW, Shaw YJ, Kulp SK, Chen CS. 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] Lee TX1, Packer MD, Huang J, Akhmametyeva EM, Kulp SK, Chen CS, Giovannini M, Jacob A, Welling DB, Chang LS. Growth inhibitory and anti-tumour activities of OSU-03012, a novel PDK-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells. Eur J Cancer. 2009 Jun;45(9):1709-20.
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PCR技术类似于DNA的天然复制过程，其特异性依赖于与靶序列两端互补的寡核苷酸引物,由变性--退火--延伸三个基本反应步骤构成
2、仪器功能：进口和国产仪器主要功能：如保存，过温保护，断电保护，热盖功能等基本上是一样的，只是附带功能上有所差别，比如：进口的显示屏是大型的触摸式荧屏操作，国产的大多是触摸键，荧屏显示操作，进口仪器有的可以升级为荧光定量PCR仪，而国产的目前主要是专用机。而这些仪器附带功能的差别大多都是最近两年新推出来的，价格确是相差几倍。有的进口仪器没有这些附带的特殊功能，从性能和功能上比有的等于或低于国产的。
普通PCR的孔所有温度是一样的。
