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    AZD-4635 (HTL1071)
    AZD-4635 (HTL1071)

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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 #: V0069
    CAS #: 1321514-06-0Purity ≥98%

    Description: AZD-4635 (also known as HTL-1071) is a novel, potent, selective, orally bioavailable small molecule inhibitor of the adenosine A2A receptor (A2AR) with Ki of 1.7 nM. It binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors. The blockade of A2aR signaling with an inhibitor such as AZD4635 can reduce tumor burden and enhance antitumor immunity. AZD4635 is currently in a Phase 1 clinical trial as a single agent and in combination with durvalumab (anti-PD-L1 Ab) in patients with solid malignancies. Accumulation of extracellular adenosine within the microenvironment is a strategy exploited by tumors to escape immunosurveillance. Adenosine signaling through the high affinity adenosine 2A receptor (A2AR) on immune cells elicits a range of immunosuppressive effects which can promote tumor growth and limit the efficacy of immune checkpoint inhibitors such as anti-PD-1 or anti-PD-L1 Abs. 

    References: AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 5580.


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    Molecular Weight (MW) 315.73
    Formula C15H11ClFN5
    CAS No. 1321514-06-0
    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 6-(2-chloro-6-methylpyridin-4-yl)-5-(4-fluorophenyl)-1,2,4-triazin-3-amine
    Synonyms HTL-1071; HTL 1071; HTL1071; AZD-4635; AZD 4635; AZD4635.
    SMILES Code NC1=NC(C2=CC=C(F)C=C2)=C(C3=CC(Cl)=NC(C)=C3)N=N1


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    In Vitro

    In vitro activity: AZD-4635 (also known as HTL-1071) is a novel, potent, selective, orally bioavailable small molecule inhibitor of the adenosine A2A receptor (A2AR) with Ki of 1.7 nM. It binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors. The blockade of A2aR signaling with an inhibitor such as AZD4635 can reduce tumor burden and enhance antitumor immunity. AZD4635 is currently in a Phase 1 clinical trial as a single agent and in combination with durvalumab (anti-PD-L1 Ab) in patients with solid malignancies. Accumulation of extracellular adenosine within the microenvironment is a strategy exploited by tumors to escape immunosurveillance. Adenosine signaling through the high affinity adenosine 2A receptor (A2AR) on immune cells elicits a range of immunosuppressive effects which can promote tumor growth and limit the efficacy of immune checkpoint inhibitors such as anti-PD-1 or anti-PD-L1 Abs. 


    Kinase Assay: It binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors. 


    Cell Assay: CHO cells stably expressing human A2AR were incubated with concentrations of adenosine ranging from 0.1 to 10 μM. In the presence of 0.1, 1 and 10 μM adenosine, the IC50 of AZD4635 for inhibition of cAMP production was 0.79, 10.0 and 142.9 nM, respectively. In an ex vivo CD8+ T cell assay, AZD4635 reversed suppression and restored IFNγ secretion in cells incubated with 5’-N-ethylcarboxamidoadenosine (NECA), a stable analog of adenosine. 

    In VivoThe therapeutic benefit of A2aR blockade was evaluated in syngeneic mouse tumor models. Inhibition of A2aR signaling led to a reduction in tumor growth alone and in combination with checkpoint inhibitors. Tumors harvested from the treated mice exhibited changes in infiltrating lymphocyte populations and increases in the functional activity of T cells. These results demonstrate that AZD4635 is a potent and selective A2aR inhibitor, and that blockade of A2aR signaling with an inhibitor such as AZD4635 can reduce tumor burden and enhance antitumor immunity. 
    Animal modelSyngeneic mouse tumor models
    Formulation & Dosage
    References AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 5580.


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

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