SML2551
AZ32
≥98% (HPLC)
别名:
N-Methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)benzamide
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
[n]21c(ncc2c4ccc(cc4)C(=O)NC)C=NC(=C1)c3ccccc3
InChI
1S/C20H16N4O/c1-21-20(25)16-9-7-15(8-10-16)18-11-23-19-12-22-17(13-24(18)19)14-5-3-2-4-6-14/h2-13H,1H3,(H,21,25)
InChI key
LCRTUEXVVKVKBD-UHFFFAOYSA-N
相关类别
生化/生理作用
AZ32 is an orally active, potent and selective ataxia telangiectasia mutated (ATM) kinase inhibitor (IC50 <6.2 nM; DNA-PK & PI3Ka IC50 =4.6 μM, hERG IC50 = 17.6 μM) with good aqueous solubility (24 μM) and blood-brain barrier (BBB) permeability in mice (free brain/plasma ratio = 0.26; 200 mg/kg p.o.). AZ32 exhibits radiosensitizing efficacy in human & murine glioma cultures by blocking radiation-induced DNA damage response (ATM pS1981 IC50 = 310 nM; 100% blockage of KAP1 pS824 & p53 pS15 at 300 nM; T98G cells). AZ32 (200 mg/kg/day p.o.) improves whole-head irradiation treatment survival rate among mice with brain GL261 tumors or NCI-H2228 NSCLC metastases in vivo.
Orally active, brain-penetrant, potent and selective ataxia telangiectasia mutated (ATM) kinase inhibitor with cancer radiosensitizing efficacy in vitro and in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
Jeremy Karlin et al.
Molecular cancer therapeutics, 17(8), 1637-1647 (2018-05-18)
Inhibition of ataxia-telangiectasia mutated (ATM) during radiotherapy of glioblastoma multiforme (GBM) may improve tumor control by short-circuiting the response to radiation-induced DNA damage. A major impediment for clinical implementation is that current inhibitors have limited central nervous system (CNS) bioavailability;
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