1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)
  3. AZD-7762

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

For research use only. We do not sell to patients.

AZD-7762 Chemical Structure

AZD-7762 Chemical Structure

CAS No. : 860352-01-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 130 In-stock
50 mg USD 366 In-stock
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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of AZD-7762:

Top Publications Citing Use of Products

    AZD-7762 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.

    View All Checkpoint Kinase (Chk) Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target[1]

    Chk1

    5 nM (IC50)

    Chk2

    5 nM (IC50)

    In Vitro

    AZD-7762 (AZD7762) is an equally potent inhibitor of Chk1 and Chk2 in vitro. AZD-7762 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 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 is determined to be 3.6 nM. Kinetic characterization suggests that AZD-7762 binds in the ATP-binding site of Chk1 and is thought to compete directly for ATP binding in a reversible manner. AZD-7762 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.

    In Vivo

    In the rat H460-DNp53 xenograft study, AZD-7762 (AZD7762) potentiates the antitumor activity of NSC 613327 in a dose-dependent manner by a decrease in %T/C with increasing dose (48% and 32%, 10 and 20 mg/kg AZD-7762, respectively). In the mouse xenograft study in combination with CPT-11, SW620 established tumors are treated with vehicle, CPT-11 alone, AZD-7762 alone, or AZD-7762 in combination with CPT-11. AZD-7762 dosed alone shows insignificant antitumor activity, whereas CPT-11 alone displays striking and significant activity (%T/C with increasing dose is 9 and 1, respectively ). In combination with AZD-7762, %T/C increases significantly to -66% and -67%, respectively[1]. AZD7762 combination with CX-5461 induces cancer cell death of Tp53-null (Tp53-/-) Eμ-Myc lymphoma cells in vitro and in vivo[2].

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

    Clinical Trial
    Molecular Weight

    362.42

    Formula

    C17H19FN4O2S

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(N[C@@H]1CNCCC1)C2=C(C=C(S2)C3=CC=CC(F)=C3)NC(N)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (275.92 mM; Need ultrasonic; 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 2.7592 mL 13.7961 mL 27.5922 mL
    5 mM 0.5518 mL 2.7592 mL 5.5184 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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    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

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% HP-β-CD

      Solubility: 10 mg/mL (27.59 mM); Clear solution; Need ultrasonic

    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.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.94%

    References
    Cell Assay
    [1]

    SW620 (5.5×103 per well) or MDA-MB-231 (5×103 per well) cells are seeded in 96-well plates and incubated overnight. Cells are dosed for 24 h with a 9-point titration of NSC 613327 ranging from 0.01 to 100 nM with or without a constant dose of AZD-7762 (300 nM). Control wells are dosed with vehicle alone (0.1% DMSO) or 300 nM AZD-7762. After 24 h, medium is removed and AZD-7762 alone is added back to the wells treated previously with AZD-7762 for an additional 24 h. Cells are then incubated in drug-free medium for an additional 72 h. The effect on cell proliferation is determined by MTS assay[1].

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

    Animal Administration
    [1][2]

    Mice and Rats[1]
    Male NCr mice and male rnu rats are used. For xenograft models in mice, tumor cells are harvested, pelleted by centrifugation for 5 min, and resuspended in sterile PBS. Cells (3×103-6×106) are implanted s.c. into the right flank of the mice in a volume of 0.1 to 0.2 mL using a 25-gauge needle. Tumors are allowed to grow to the designated size of 100 to 200 mm3 before the administration of compound. For xenograft models in rats, Cells are harvested, pelleted by centrifugation for 5 min, and resuspended in 50% sterile PBS and 50% Matrigel. Rats receive a 5 Gy whole-body radiation dose 5 days before cell implantation to improve tumor growth. H460-DNp53 cells (1×107) are implanted s.c., into the right flank of the rats in a volume of 0.2 mL using a 25-gauge needle. Tumors are allowed to grow to the designated size of 100 to 200 mm3 before the administration of AZD-7762. AZD-7762 (10 and 20 mg/kg) is administered by i.v. injection via the tail vein. Cyclic schedules are used and treatment ranged from three to five cycles. Each cycle includes administration of a standard agent (NSC 613327 or CPT-11) every 3 days follow by delivery of AZD-7762. Tumor volumes are measured with electronic calipers and calculated.
    Mice [2]
    C57Bl/6 mice are intravenously injected with 2×105 Eμ-Myc B-lymphoma cells in PBS and treated with pharmacological inhibitors from 8 days post-injection. Treatment of mice is continued until an ethical end-point is reached; hunched posture, ruffled fur, enlarged lymph nodes, laboured breathing, weight loss greater than 20% of start body weight and limited mobility or paralysis. AZD7762 is delivered intraperitoneally in 10.3% -hydroxypropyl-β-cyclodextrin in 0.9% saline at 20 mg/kg daily on weekdays.

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

    References

    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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. 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 2.7592 mL 13.7961 mL 27.5922 mL 68.9804 mL
    5 mM 0.5518 mL 2.7592 mL 5.5184 mL 13.7961 mL
    10 mM 0.2759 mL 1.3796 mL 2.7592 mL 6.8980 mL
    15 mM 0.1839 mL 0.9197 mL 1.8395 mL 4.5987 mL
    20 mM 0.1380 mL 0.6898 mL 1.3796 mL 3.4490 mL
    25 mM 0.1104 mL 0.5518 mL 1.1037 mL 2.7592 mL
    30 mM 0.0920 mL 0.4599 mL 0.9197 mL 2.2993 mL
    40 mM 0.0690 mL 0.3449 mL 0.6898 mL 1.7245 mL
    50 mM 0.0552 mL 0.2759 mL 0.5518 mL 1.3796 mL
    60 mM 0.0460 mL 0.2299 mL 0.4599 mL 1.1497 mL
    80 mM 0.0345 mL 0.1725 mL 0.3449 mL 0.8623 mL
    100 mM 0.0276 mL 0.1380 mL 0.2759 mL 0.6898 mL
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    AZD-7762 Related Classifications

    Help & FAQs
    • 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.

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