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> AZD1390 [2089288-03-7]

AZD1390 [2089288-03-7]

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Referentie HY-109566-10mg

Formaat : 10mg

Merk : MedChemExpress

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

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

AZD1390 Chemical Structure

AZD1390 Chemical Structure

CAS No. : 2089288-03-7

This product is a controlled substance and not for sale in your territory.

Based on 6 publication(s) in Google Scholar

Voir tous les produits spécifiques à Isoform ATM/ATR:

Voir toutes les isoformes
ATM ATR
Description

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

 

Cellular Effect
Cell Line Type Value Description References
HT-29 IC50
> 10 μM
Compound: AZD1390
Cytotoxicity against ATM proficient human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against ATM proficient human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 35183872]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
Masse moléculaire

477.57

Formule

C27H32FN5O2
CAS No.

2089288-03-7
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C(C)C)N(C)C2=C1C3=CC(C4=CC=C(OCCCN5CCCCC5)N=C4)=C(F)C=C3N=C2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvant et solubilité
In Vitro: 

DMSO : 5 mg/mL (10.47 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureté et documentation

Purity: 99.28%

SDS (393 KB)

COA (247 KB) LCMS (96 KB)

Instruction de manipulation (2659 KB)
Références

  • [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.  [Content Brief]

    [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.

Administration animale
[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].

MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références

  • [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.  [Content Brief]

    [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.

  • [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.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0939 mL 10.4697 mL 20.9393 mL 52.3483 mL
5 mM 0.4188 mL 2.0939 mL 4.1879 mL 10.4697 mL
10 mM 0.2094 mL 1.0470 mL 2.0939 mL 5.2348 mL
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AZD1390 Related Classifications

  • Cell Cycle/DNA Damage PI3K/Akt/mTOR
  • ATM/ATR
Help & FAQs

Keywords:

AZD13902089288-03-7AZD 1390AZD-1390ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedInhibitorinhibitorinhibit