2. AZD-7762 hydrochloride

AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.

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AZD-7762 hydrochloride Chemical Structure

AZD-7762 hydrochloride Chemical Structure

CAS No. : 1246094-78-9

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AZD-7762 hydrochloride Related Antibodies

Top Publications Citing Use of Products

    AZD-7762 hydrochloride purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Jan 18;12(1):e0170308.  [Abstract]

    Inhibition of nuclear actin filament formation by Chek1/2 inhibitor, AZD7762 (AZD). No nuclear actin filament formation is observed upon treatment of CEOs with AZD alone.

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    Description

    AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.

    IC50 & Target

    IC50: 5 nM (ChK1), 5 nM (ChK2)[1]
    In Vitro

    AZD-7762 hydrochloride (AZD7762) is an equally potent inhibitor of Chk1 and Chk2 in vitro. AZD-7762 hydrochloride potently inhibits Chk1 and Chk2, abrogates DNA damage-induced S and G2 checkpoints, enhances the efficacy of NSC 613327 and SKF 104864A, and modulates downstream checkpoint pathway proteins. AZD-7762 hydrochloride potently inhibits Chk1 phosphorylation of a cdc25C peptide with an IC50 of 5 nM as measured by a scintillation proximity assay. The Ki for AZD-7762 hydrochloride is determined to be 3.6 nM. Kinetic characterization suggests that AZD-7762 hydrochloride binds in the ATP-binding site of Chk1 and is thought to compete directly for ATP binding in a reversible manner. AZD-7762 hydrochloride is shown to abrogate the G2 arrest induced by Camptothecin with an average EC50 of 10 nM (n=12) and maximal abrogation in the range of 100 nM[1].

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

    AZD-7762 hydrochloride Related Antibodies
    In Vivo

    In rat H460-DNp53 xenograft studies, AZD-7762 hydrochloride (10 mg/kg and 20 mg/kg) potentiates the antitumor activity of NSC 613327 in a dose-dependent manner. That is, the inhibition rate (%T/C) decreases to 48% and 32%, respectively, with increasing dose. In a mouse xenograft study in combination with CPT-11, treatment with AZD-7762 hydrochloride in combination with CPT-11 significantly increased CPT-11 activity with a significant increase in %T/C to -66% and -67%, respectively[1]. AZD7762 hydrochloride in combination with CX-5461 induces Tp53-null (Tp53-/-) Eμ-Myc in vitro and in vivo Lymphoma cell death[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    398.88

    Formula

    C17H20ClFN4O2S
    CAS No.
    SMILES

    O=C(C1=C(NC(N)=O)C=C(C2=CC=CC(F)=C2)S1)N[C@@H]3CNCCC3.Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    AZD-77621246094-78-9AZD7762AZD 7762Inhibitorinhibitorinhibit

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