431979-47-4
中文名稱
CS-1226
英文名稱
2-[2-Chloro-4-[(1,5-dihydro-3-methyl-5-oxo-1-phenyl-4H-pyrazol-4-ylidene)methyl]-6-ethoxyphenoxy]aceticacidmethylester
CAS
431979-47-4
分子式
C22H21ClN2O5
分子量
428.87
MOL 文件
431979-47-4.mol
更新日期
2024/11/15 18:20:34
431979-47-4 結(jié)構(gòu)式
基本信息
中文別名
化合物SJ-172550MDMX小分子抑制劑(SJ-172550)
英文別名
CS-1226SJ 172550
MDMX Antagonist, SJ-172550
MDMX Antagonist, SJ-172550 - CAS 431979-47-4 - Calbiochem
2-[2-Chloro-4-[(1,5-dihydro-3-methyl-5-oxo-1-phenyl-4H-pyrazol-4-ylidene)methyl]-6-ethoxyphenoxy]aceticacidmethylester
Acetic acid, 2-[2-chloro-4-[(1,5-dihydro-3-methyl-5-oxo-1-phenyl-4H-pyrazol-4-ylidene)methyl]-6-ethoxyphenoxy]-, methyl ester
所屬類別
生物化工：抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)560.8±60.0 °C(Predicted)
密度1.27±0.1 g/cm3(Predicted)
儲存條件Sealed in dry,2-8°C
溶解度二甲基亞砜：≥30mg/mL
酸度系數(shù)(pKa)-0.30±0.40(Predicted)
形態(tài)粉末
顏色橙色
常見問題列表
生物活性
SJ-172550是MDMX的小分子抑制劑; 與野生型p53肽競爭性結(jié)合于MDMX的EC50值為5 μM。靶點(diǎn)
IC50: 5 μM (MDMX)
體外研究
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.