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CAS No.: 702674-56-4

BX-912 Catalog No. CSN17175

BX-912 is a selective inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1) with IC50 of 12 nM, showing > 10 fold selectivity over PKA, PKC, C-Kit, EGFR etc.

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400-920-2911

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tech@csnpharm.cn

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400-920-2911

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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

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. 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. 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.
作用机制BX-912 binds to the ATP binding pocket of PDK1. The structure of enzyme-inhibitor complexes reveals two hydrogen bonds between two aminopyrimidine nitrogens and the amino acid backbone of Ala¹⁶², which lies in the hinge region of the molecule.

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
- 2.1215 mL
- 10.6077 mL
- 21.2155 mL
- 5 mM
- 0.4243 mL
- 2.1215 mL
- 4.2431 mL
- 10 mM
- 0.2122 mL
- 1.0608 mL
- 2.1215 mL

技术信息

CAS号

702674-56-4

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H23BrN8O

运输

蓝冰

分子量

471.35

别名

溶解度

DMSO	100.0 mg/mL (212.2 mM)

动物实验配方

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BX-912 Catalog No. CSN17175

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