产品说明书

BX795

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Chemical Structure| 702675-74-9 同义名 : -
CAS号 : 702675-74-9
货号 : A700044
分子式 : C23H26IN7O2S
纯度 : 99%+
分子量 : 591.468
MDL号 : MFCD12546134
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(59.17 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG +2% Tween 80+water 4 mg/mL

生物活性
靶点

  • PDK1

    PDK-1, IC50:6 nM
描述 The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and represents a promising target for anticancer drugs[3]. BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor with an IC50 value of 26 nM. BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis[3]. When treating asynchronously growing cultures of tumor cells for 18 h with 10 μM BX-912, it promoted a pronounced increase in the population of MDA-468 cells with 4 N DNA content, indicative of a block at the G2/M phase of the cell cycle. BX-912 also potently inhibited the growth of HCT-116 and PC-3 cells in soft agar, showing a 96% inhibitory effect at a dose of 1 μM for HCT-116 and IC50 value of 0.32 μM for PC-3[3].
作用机制 BX-795 is a competitive inhibitor of PDK1 activity with respect to its substrate, ATP, suggesting that it binds to the ATP binding pocket of PDK1[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human 5637 cell Growth inhibition assay Inhibition of human 5637 cell growth in a cell viability assay, IC50=8.07904 μM SANGER
human 697 cell Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=1.01623 μM SANGER
human 8-MG-BA cell Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=1.95744 μM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.69mL

0.34mL

0.17mL

8.45mL

1.69mL

0.85mL

16.91mL

3.38mL

1.69mL
参考文献

[1]Feldman RI, Wu JM, Polokoff MA, Kochanny MJ, Dinter H, Zhu D, Biroc SL, Alicke B, Bryant J, Yuan S, Buckman BO, Lentz D, Ferrer M, Whitlow M, Adler M, Finster S, Chang Z, Arnaiz DO. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. doi: 10.1074/jbc.M501367200. Epub 2005 Mar 16. PMID: 15772071.