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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PDK1-PDK1 inhibitor AR12
PDK1 inhibitor AR12

Chemical Structure : PDK1 inhibitor AR12

CAS No.: 742112-33-0

PDK1 inhibitor AR12 (AR-12, OSU-03012, OSU03012)

货号: PC-60605Not For Human Use, Lab Use Only.

OSU-03012 (AR12) is a potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) inhibitor with IC50 of 5 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

OSU-03012 (AR12) is a potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) inhibitor with IC50 of 5 uM.
OSU-03012 induces apoptosis in PC-3 cells at low microM range, causes Akt dephosphorylation and inhibition of p70 S6 kinase activity;.
OSU-03012 displays cytotocixity against a panel of 60 cell lines with mean GI50 of 3 uM.
OSU-03012 decreases incidences of carcinoma and metastasis in transgenic mouse model of prostate cancer.

物理化学性质&存储条件

分子量 460.46
分子式 C26H19F3N4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-phenyl} acetamide

参考文献

1. Johnson AJ, et al. Blood. 2005 Mar 15;105(6):2504-9.

2. Tseng PH, et al. Blood. 2005 May 15;105(10):4021-7.

3. Zhu J, et al. Cancer Res. 2004 Jun 15;64(12):4309-18.

4. Baryawno N, et al. Cancer Res. 2010 Jan 1;70(1):266-76.

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