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2288709-96-4

中文名稱(chēng) Benzamide, N-methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)-
英文名稱(chēng) AZ32
CAS 2288709-96-4
分子式 C20H16N4O
分子量 328.37
MOL 文件 2288709-96-4.mol
更新日期 2025/01/22 01:49:23
2288709-96-4 結(jié)構(gòu)式 2288709-96-4 結(jié)構(gòu)式

基本信息

中文別名
N-甲基-4-(6-苯基咪唑[1,2-A]吡嗪-3-)苯甲酰胺
英文別名
N-Methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)benzamide
Benzamide, N-methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)-

物理化學(xué)性質(zhì)

密度1.25±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 150 mg/ml
酸度系數(shù)(pKa)14.63±0.46(Predicted)
形態(tài)固體
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P305+P351+P338

圖譜信息

常見(jiàn)問(wèn)題列表

生物活性
AZ32 是一種口服可利用的，可穿透血腦屏障的 ATM 抑制劑，IC50<6.2 nM。在細(xì)胞中抑制 ATM，IC50 為 0.31 μM。
靶點(diǎn)

ATM

6.2 nM (IC 50 )

ATM

0.31 μM (IC 50 , in cell)

體外研究

AZ32 is a next-generation blood-brain barrier (BBB)-penetrating ATM inhibitor. AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro.

體內(nèi)研究

AZ32, with enhanced BBB penetration, is highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model compared with AZ31. AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse. Following a single oral dose of AZ32 (200 mg/kg) in mice, the free-brain concentrations of AZ32 are in excess of the cellular IC 50 for approximately 22 hours.

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