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AZD1390 ATM inhibitor

Name: AZD1390
Brand: Selleck Chemicals
SKU: S8680
Availability: InStock
Rating: 5 (25 reviews)

Cat.No.S8680

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.

Chemical Structure

Molecular Weight: 477.57

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	PI3K Akt mTOR GSK-3 DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other ATM/ATR Inhibitors	KU-60019 Berzosertib (VE-822) Ceralasertib (AZD6738) Camonsertib (RP-3500) Lartesertib (M4076) KU-55933 VE-821 AZ20 AZD0156 Mirin

Solubility

In vitro
Batch:

Ethanol : 95 mg/mL

DMSO : 14 mg/mL (29.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 40%PEG300 2 5%TWEEN80 3 45%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.500mg/ml (3.14mM)	Taking the 1 mL working solution as an example, add 100 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	477.57	Formula	C₂₇H₃₂FN₅O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2089288-03-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)N1C2=C(C=NC3=CC(=C(C=C32)C4=CN=C(C=C4)OCCCN5CCCCC5)F)N(C1=O)C

Mechanism of Action

Targets/IC₅₀/Ki	ATM (Cell-based assay) 0.78 nM
In vitro	AZD1390 blocks ATM-dependent DDR (DNA damage response) pathway activity and combines with radiation to induce G2 cell cycle phase accumulation, micronuclei, and apoptosis. This compound radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type. It results in increased genome instability.
In vivo	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 this compound with radiotherapy, compared to radiotherapy treatment alone. In in vivo syngeneic and patient-derived glioma as well as orthotopic lung-brain metastatic models, this compound 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. This compound has favorable physical, chemical, PK, and PD properties suitable for clinical applications that require exposures within the central nervous system.
References	[1] http://mct.aacrjournals.org/content/17/1_Supplement/A124 [2] http://advances.sciencemag.org/content/4/6/eaat1719

Applications

Methods	Biomarkers	Images	PMID
Western blot	pChk2 pATM (S1981) / ATM / pKAP1(S824) / KAP1 / pCDK1		29938225

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05182905	Recruiting	Glioblastoma\|Glioma\|Glioblastoma Multiforme\|Glioma Malignant	Nader Sanai\|Barrow Neurological Institute\|Ivy Brain Tumor Center\|AstraZeneca\|St. Joseph''s Hospital and Medical Center Phoenix	March 9 2022	Early Phase 1
NCT03423628	Recruiting	Recurrent Glioblastoma Multiforme\|Primary Glioblastoma Multiforme\|Brain Neoplasms Malignant\|Leptomeningeal Disease (LMD)	AstraZeneca	April 2 2018	Phase 1
NCT03215381	Completed	Healthy Volunteer Male Subjects	AstraZeneca\|Karolinska Institutet Quintiles IMS	October 10 2017	Phase 1

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Handling Instructions

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