AZD1390
目录号 : GC19468
AZD1390 是一种强效、高选择性、口服生物可利用的脑渗透性 ATM 抑制剂，在细胞中的 IC50 为 0.78 nM。
Cas No.:2089288-03-7
Sample solution is provided at 25 µL, 10mM.
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AZD1390 is a potent and selective ATM inhibitor with the ability to cross the blood-brain barrier suitable for the treatment of intracranial malignancies.AZD1390 is an exceptionally potent inhibitor of ATM in cells (IC50 = 0.78 nM) with >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.
AZD1390 displays excellent oral bioavailability in preclinical species (66% in rat and 74% in dog), is not a substrate for human efflux transporters, and has been shown to efficiently cross the BBB in non-human primate PET studies.
Reference:
http://mct.aacrjournals.org/content/17/1_Supplement/A124
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 2089288-03-7 | SDF | |
| 化学名 | 7-fluoro-1-isopropyl-3-methyl-8-(6-(3-(piperidin-1-yl)propoxy)pyridin-3-yl)-1H-imidazo[4,5-c]quinolin-2(3H)-one | ||
| Canonical SMILES | FC(C=C(N=CC(N1C)=C2N(C(C)C)C1=O)C2=C3)=C3C(C=N4)=CC=C4OCCCN5CCCCC5 | ||
| 分子式 | C27H32FN5O2 | 分子量 | 477.57 |
| 溶解度 | DMSO : 5 mg/mL (10.47 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 | 1.047 mL | 2.0939 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet