|2-氨基-N-[4-[5-(2-菲基)-3-(三氟甲基)-1H-吡唑-1-基]苯基]乙酰胺|CsnPharm

CAS No.: 742112-33-0

2-Amino-N-(4-(5-(phenanthren-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)acetamide Catalog No. CSN12988

Synonyms: AR-12

OSU-03012 is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PDK-1

IC50:5μM
描述3'-Phosphoinositide-dependent protein kinase 1 (PDK-1) phosphorylates and activates members of the AGC protein kinase family and plays an important role in the regulation of cell survival, differentiation, and proliferation^[3]. OSU-03012 is a PDK-1 inhibitor with an IC₅₀ of 5 μM. OSU-03012 induces apoptotic death in PC-3 cells in 1% FBS-containing medium in a dose-dependent manner, as demonstrated by DNA fragmentation and PARP cleavage. It is effective in suppressing PC-3 cell proliferation at sub-μM, consistent with that noted in 1% serum. OSU-03012 was able to completely suppress cell growth in a diverse range of tumor cell lines at the 3-5 μM therapeutic range, as compared with the concentration of at least 50 μM required for celecoxib^[4]. OSU-03012 inhibited cell growth of Huh7, Hep3B, and HepG2 cells with IC₅₀ below 1 mumol/L^[5]. Daily oral treatment of BALB/c nude mice with OSU-03012 suppressed the growth of Huh7 tumor xenografts. Electron microscopic observation indicated that OSU-03012 induced autophagy in vivo^[5]. OSU-03012 remarkably decreases EGFR protein expression in the tumors by ~48% compared with expression levels found in the tumors taken from mice that receive the vehicle control. OSU-03012 also prevents Y-box binding protein-1 (YB-1) from binding to the EGFR promoter at the 1b and 2a sites^[6].
作用机制The guanidino group of OSU-03012 resembled the partial structure of the purine ring of ATP, which allowed the formation of hydrogen bonds with Ser160 and Ala162 as depicted by the docking model.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
mouse RAW264.7 cells	-	Function assay	8 h	Antimicrobial activity against Salmonella enterica serovar Typhimurium ATCC 14028 infected in mouse RAW264.7 cells assessed as inhibition of intracellular bacterial growth after 8 hrs, IC50=0.2 μM	19805568
mouse RAW264.7 cells	-	Cytotoxic assay	24 h	Cytotoxicity against mouse RAW264.7 cells assessed as cell viability after 24 hrs by MTT assay, IC50=10 μM	19805568

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1718 mL
- 10.8589 mL
- 21.7179 mL
- 5 mM
- 0.4344 mL
- 2.1718 mL
- 4.3436 mL
- 10 mM
- 0.2172 mL
- 1.0859 mL
- 2.1718 mL

技术信息

CAS号

742112-33-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H19F3N4O

运输

蓝冰

分子量

460.45

别名

AR-12

溶解度

DMSO	11.0 mg/mL (23.9 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

0.5% methylcellulose+0.2% Tween 80+water

30 mg/mL

suspension

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2-Amino-N-(4-(5-(phenanthren-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)acetamide Catalog No. CSN12988

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