中文名称:

CS-1226

中文同义词:

MDMX小分子抑制剂(SJ-172550);化合物SJ-172550

英文名称:

2-[2-Chloro-4-[(1,5-dihydro-3-methyl-5-oxo-1-phenyl-4H-pyrazol-4-ylidene)methyl]-6-ethoxyphenoxy]aceticacidmethylester

英文同义词:

2-[2-Chloro-4-[(1,5-dihydro-3-methyl-5-oxo-1-phenyl-4H-pyrazol-4-ylidene)methyl]-6-ethoxyphenoxy]aceticacidmethylester;SJ 172550;MDMX Antagonist, SJ-172550;CS-1226;MDMX Antagonist, SJ-172550 - CAS 431979-47-4 - Calbiochem;Acetic acid, 2-[2-chloro-4-[(1,5-dihydro-3-methyl-5-oxo-1-phenyl-4H-pyrazol-4-ylidene)methyl]-6-ethoxyphenoxy]-, methyl ester

CAS号:

431979-47-4

分子式:

C22H21ClN2O5

分子量:

428.87

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

431979-47-4.mol

沸点 

560.8±60.0 °C(Predicted)

密度 

1.27±0.1 g/cm3(Predicted)

储存条件 

Sealed in dry,2-8°C

溶解度 

DMSO: ≥30mg/mL

形态

powder

酸度系数(pKa)

-0.30±0.40(Predicted)

颜色

orange

生物活性

SJ-172550是MDMX的小分子抑制剂; 与野生型p53肽竞争性结合于MDMX的EC50值为5 μM。

靶点

IC50: 5 μM (MDMX)

体外研究

The p53 pathway is disrupted in virtually every human tumor. SJ-172550 binds the p53-binding pocket of MDMX, thereby displacing p53. SJ-172550 binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified. The effect of SJ-172550 is additive when combined with an MDM2 inhibitor nutlin-3a. SJ-172550 acts through a complicated mechanism in which the compound forms a covalent but reversible complex with MDMX and locks MDMX into a conformation that is unable to bind p53. The relative stability of this complex is influenced by many factors including the reducing potential of the media, the presence of aggregates.

危险品标志 

Xn

危险类别码 

22

WGK Germany 

3