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AZD1390

Catalog No.GC19468

AZD1390 is a potent and selective ATM inhibitor

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AZD1390 Chemical Structure

Cas No.: 2089288-03-7

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5mg
$126.00
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10mg
$202.00
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50mg
$714.00
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500mg
$2,627.00
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1g
$4,202.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

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.
[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.

Background

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

Chemical Properties

Cas No. 2089288-03-7 SDF
Chemical Name 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
Formula C27H32FN5O2 M.Wt 477.57
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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