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  • AZD1390

    • AZD-1390;AZD 1390
    货号: abs811990
    CAS号: 2089288-03-7
    分子式: C27H32FN5O
    分子量: 477.57
    产品说明书
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    货号-规格 货期 价格 数量
    abs811990-5mg 1-2周 ¥1874.00
    - +
    abs811990-25mg 1-2周 ¥5858.00
    - +
    大包装询价
    产品描述
    描述

    AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    AZD-1390;AZD 1390
    外观
    powder
    可溶性/溶解性
    DMSO :14 mg/mL (29.32 mM)
    生物活性
    靶点
    ATM
    In vitro(体外研究)
    AZD1390 blocks ATM-dependent DDR (DNA damage response) pathway activity and combines with radiation to induce G2 cell cycle phase accumulation, micronuclei, and apoptosis. AZD1390 radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type. AZD1390 results in increased genome instability.
    In vivo(体内研究)
    AZD1390 displays excellent oral bioavailability in preclinical species (66% in rat and 74% in dog). It can efficiently cross the BBB in non-human primate PET studies. Profound tumor regressions and increased animal survival (>50 days) have been observed in orthotopic xenograft models of brain cancer following just 2 or 4 days combination treatment of AZD1390 with radiotherapy, compared to radiotherapy treatment alone. In in vivo syngeneic and patient-derived glioma as well as orthotopic lung-brain metastatic models, AZD1390 dosed in combination with daily fractions of IR (whole-brain or stereotactic radiotherapy) significantly induces tumor regressions and increased animal survival compared to IR treatment alone. AZD1390 has favorable physical, chemical, PK, and PD properties suitable for clinical applications that require exposures within the central nervous system.
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