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    AZD1390
    AZD1390

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0075
    CAS #: 2089288-03-7Purity ≥98%

    Description: AZD1390 (AZD-1390) is a novel, potent, selective, first-in-class orally bioavailable and CNS penetrant inhibitor of Ataxia-telangiectasia mutated (ATM) kinase with potential anticancer activity. It has an IC50 of 0.78 nM for inhibiting ATM in cell assays, and is >10,000-fold more selective over closely related PIKK family of enzymes and excellent selectivity across a broad range of kinases. AZD1390 is able to cross the blood-brain barrier (BBB) which makes it suitable for the treatment of intracranial malignancies. AZD1390 radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type. AZD1390 is now in early clinical development for use as a radiosensitizer in central nervous system malignancies.

    References: Science Advances. 2018, 4(6): eaat1719


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    Molecular Weight (MW) 477.57
    Formula C27H32FN5O2
    CAS No. 2089288-03-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: > 10mM
    Water: N/A
    Ethanol: N/A
    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
    Synonyms AZD-1390; AZD1390; AZD 1390
    SMILES Code O=C(N1C(C)C)N(C)C2=C1C3=CC(C4=CC=C(OCCCN5CCCCC5)N=C4)=C(F)C=C3N=C2


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    In Vitro

    In vitro activity: AZD1390 is a novel, potent, selective, first-in-class orally bioavailable and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cell assays. It is >10,000-fold more selective over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases. AZD1390 has the ability to cross the blood-brain barrier (BBB) which makes it suitable for the treatment of intracranial malignancies. AZD1390 radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type. AZD1390 is now in early clinical development for use as a radiosensitizer in central nervous system malignancies.


    Kinase Assay: AZD1390 is a novel, potent, selective, first-in-class orally bioavailable and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cell assays. It is >10,000-fold more selective over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.  


    Cell Assay: 3000 Cells are seeded into each well of a 384-well plate in RPMI with 10% fetal bovine serum. After 24 hours, plates are Echo-dosed with a semi-log dose dilution of each compound from a top concentration of 1250 nM. One hour after compound dosing, plates are irradiated with 0, 2.5, or 4 Gy. At 1, 6, 24, and 48 hours after irradiation, plates are fixed by adding a 1:1 volume of 8% PFA directly to the medium to give a final concentration of 4% PFA and incubated for 30 min at room temperature before washing three times with phosphate-buffered saline solution (PBSA). 

    In VivoAZD1390 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 AZD1390 with radiotherapy, compared to radiotherapy treatment alone. In in vivo syngeneic and patient-derived glioma as well as orthotopic lung-brain metastatic models, AZD1390 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. AZD1390 has favorable physical, chemical, PK, and PD properties suitable for clinical applications that require exposures within the central nervous system
    Animal model Lung NCI-H2228 xenograft mice model either by implanting into nude mice brains directly (intracranial brain) or injecting into the carotid artery [intracarotid artery (ICA)]
    Formulation & Dosage Dissolved in 0.5%(w/v)HPMC, and 0.1%(w/v) Tween 80; 5, 15 and 20 mg/kg; Oral gavage
    References Science Advances. 2018, 4(6): eaat1719


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    AZD1390

    The structure and brain-penetrating properties of AZD1390. Science Advances. 2018, 4(6): eaat1719.

      

    AZD1390

    Target engagement and cellular mechanism of action of AZD1390. Science Advances. 2018, 4(6): eaat1719.

     

    AZD1390

    In vivo activity of AZD1390 in lung-brain metastatic models. Science Advances. 2018, 4(6): eaat1719.

     

    AZD1390

    Survival of a syngeneic mouse model of GBM treated with AZD1390. Science Advances. 2018, 4(6): eaat1719.

     AZD1390

    In vivo subcutaneous efficacy studies using PDX models. Science Advances. 2018, 4(6): eaat1719.

     

    AZD1390

    harmacokinetics and pharmacodynamics of AZD1390. Science Advances. 2018, 4(6): eaat1719.


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