AZD1390

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AZD1390  纯度: 99.97%

AZD1390 是一种有效的，高度选择性的，口服生物利用的，可渗透脑的 ATM 抑制剂，在细胞中对 ATM 的 IC50 为 0.78 nM。

AZD1390

AZD1390 Chemical Structure

CAS No. : 2089288-03-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1839 In-stock
1 mg ￥990 In-stock
5 mg ￥1750 In-stock
10 mg ￥2800 In-stock
25 mg ￥5400 In-stock
50 mg ￥9900 In-stock
100 mg   询价  
200 mg   询价  

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生物活性

AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM in cell[1].

IC50 & Target[1]

ATM

 

体内研究
(In Vivo)

Median survival of mice treated with AZD1390 and radiation are significantly longer than untreated control mice (p=0.001). No overt signs of treatment toxicity are observed with small animal radiation research platform (SARRP) contrary to wholehead irradiated mice that seem to develop mucositis and difficulties drinking and eating at doses >10 Gy in combination with AZD1390[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

477.57

Formula

C27H32FN5O2
CAS 号

2089288-03-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (52.35 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0939 mL 10.4697 mL 20.9393 mL
5 mM 0.4188 mL 2.0939 mL 4.1879 mL
10 mM 0.2094 mL 1.0470 mL 2.0939 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Durant ST, et al. The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models. Sci Adv. 2018 Jun 20;4(6):eaat1719.

    [2]. J. Kahn, et al. Next-Generation ATM Kinase Inhibitors Under Development Radiosensitize Glioblastoma With Conformal Radiation in a Mouse Orthotopic Model. IJROBP. 2017. 99, 600-601.
Animal Administration
[2]

Mouse GL261 glioma (p53 mutant) cells are implanted intra-cranially into immunocompetent, syngeneic C57/bl6 mice followed by bioluminescent imaging (BLI) prior to randomization. AZD1390 is administered by oral gavage prior to deliver multiple fractions of 2-3 Gy of radiation on 2 to 4 consecutive days. Radiation is administered via small animal radiation research platform (SARRP) irradiation to the site of the tumor with a 5×5 mm lateral field[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Durant ST, et al. The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models. Sci Adv. 2018 Jun 20;4(6):eaat1719.

    [2]. J. Kahn, et al. Next-Generation ATM Kinase Inhibitors Under Development Radiosensitize Glioblastoma With Conformal Radiation in a Mouse Orthotopic Model. IJROBP. 2017. 99, 600-601.

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