2. Cell Cycle/DNA Damage
  3. Wee1
  4. Adavosertib

Adavosertib  (Synonyms: AZD1775; MK-1775)

Cat. No.: HY-10993 Purity: 99.97%
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Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC50 of 5.2 nM.

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

Adavosertib Chemical Structure

Adavosertib Chemical Structure

CAS No. : 955365-80-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 46 publication(s) in Google Scholar

Other Forms of Adavosertib:

Adavosertib Related Antibodies

Top Publications Citing Use of Products

43 Publications Citing Use of MCE Adavosertib

WB

    Adavosertib purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 1;11(1):99.  [Abstract]

    Representative immunoblots showing the expression of key proteins of the WEE1 pathway after treatment with AZD-1775 (IC50 for each cell line) for 24 h of the indicated cells lines. β-actin is used for loading normalization.

    Adavosertib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2017 Sep 1;77(17):4663-4672.  [Abstract]

    Isogenic A549 or H2030 cells expressing full-length LKB1 or kinase-dead LKB1(KDLKB1) are treated with 1 μM AZD1775 or vehicle (DMSO) for 24 hours. Protein lysates are immunoblotted with the indicated antibodies. Actin was used as a loading control.

    Adavosertib purchased from MedChemExpress. Usage Cited in: Scienze biomediche. University of Bologna. 2016 Apr.

    In the blots B-/T-ALL cell lines are incubated for 24 hours with MK-1775 (IC50 value). The homogeneity of the protein loaded (40 μg) is determined using an internal control (β-actin).

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC50 of 5.2 nM.

    IC50 & Target

    IC50: 5.2 nM (Wee1)
    Cellular Effect
    Cell Line Type Value Description References
    A-427 IC50
    158 nM
    Compound: 1; AZD1775
    Antiproliferative activity against human A-427 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay
    Antiproliferative activity against human A-427 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay
    		[PMID: 37197456]
    A-427 IC50
    78 nM
    Compound: AZD1775
    Antiproliferative activity against human A-427 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay
    Antiproliferative activity against human A-427 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay
    		[PMID: 34423975]
    BT-549 IC50
    0.49 μM
    Compound: 1; AZD1775
    Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    		[PMID: 35231578]
    Daoy IC50
    150 nM
    Compound: Adavosertib
    Antiproliferative activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay
    Antiproliferative activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay
    		[PMID: 33636537]
    HEK-293T IC50
    0.29 μM
    Compound: MK-1775
    Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay
    Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay
    		[PMID: 28792760]
    LNCaP IC50
    0.5 μM
    Compound: 1; AZD1775
    Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    		[PMID: 35231578]
    MCF7 IC50
    1.1 μM
    Compound: 1; AZD1775
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    		[PMID: 35231578]
    MDA-MB-231 IC50
    0.26 μM
    Compound: MK-1775
    Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay
    Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay
    		[PMID: 28792760]
    MM1.S IC50
    0.31 μM
    Compound: MK-1775
    Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay
    Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay
    		[PMID: 28792760]
    MV4-11 IC50
    95 nM
    Compound: AZD1775
    Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Celltiter-glo assay
    Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Celltiter-glo assay
    		[PMID: 37167712]
    NCI-H1299 IC50
    0.2837 nM
    Compound: AZD-1775; MK-1775
    Inhibition of cell proliferation in human NCI-H1299 cells incubated for 3 days by MTT assay
    Inhibition of cell proliferation in human NCI-H1299 cells incubated for 3 days by MTT assay
    		[PMID: 35051747]
    NCI-H1299 IC50
    104 nM
    Compound: AZD1775
    Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition incubated for 3 days by CellTiter-Glo Luminescent assay
    Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition incubated for 3 days by CellTiter-Glo Luminescent assay
    		[PMID: 36075370]
    NCI-H23 IC50
    122 nM
    Compound: AZD1775
    Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 4 days by CellTiter-Glo assay
    Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 4 days by CellTiter-Glo assay
    		[PMID: 34423975]
    NCI-H23 IC50
    175 nM
    Compound: 1; AZD1775
    Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay
    Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay
    		[PMID: 37197456]
    PC-3 IC50
    8 μM
    Compound: 1; AZD1775
    Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    		[PMID: 35231578]
    T47D IC50
    12780 nM
    Compound: AZD1775
    Antiproliferative activity against human T47D cells incubated for 72 hrs by Celltiter-glo assay
    Antiproliferative activity against human T47D cells incubated for 72 hrs by Celltiter-glo assay
    		[PMID: 37167712]
    In Vitro

    Adavosertib (MK-1775) enhances the cytotoxic effects of 5-FU in p53-deficient human colon cancer cells. Adavosertib (MK-1775) inhibits CDC2 Y15 phosphorylation in cells, abrogates DNA damaged checkpoints induced by 5-FU treatment, and causes premature entry of mitosis determined by induction of Histone H3 phosphorylation[1].
    Adavosertib (MK-1775) abrogates the radiation-induced G2 block in p53-defective cells but not in p53 wild-type lines[2].
    The combination of NSC 613327 with Adavosertib (MK-1775) produces robust anti-tumor activity and remarkably enhances tumor regression response (4.01 fold) compared to NSC 613327 treatment in p53-deficient tumors[3].

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

    Adavosertib Related Antibodies
    In Vivo

    In vivo, Adavosertib (MK-1775) potentiates the anti-tumor efficacy of 5-FU at tolerable doses[1].
    Adavosertib (MK-1775) (60 mg/kg twice daily, p.o.) enhances H1299 xenograft tumor response to fractionated radiotherapy[2].
    Adavosertib (MK-1775) (30 mg/kg. p.o.) regresses tumor growth in PANC198, PANC215 and PANC185 as compared to GEM treated mice[3].

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

    500.60

    Formula

    C27H32N8O2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1N(N(C2=NC(NC3=CC=C(C=C3)N4CCN(CC4)C)=NC=C21)C5=NC(C(O)(C)C)=CC=C5)CC=C
    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 : 125 mg/mL (249.70 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 1.9976 mL 9.9880 mL 19.9760 mL
    5 mM 0.3995 mL 1.9976 mL 3.9952 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.87 mg/mL (5.73 mM); Clear solution

    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    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:  0.5% Methylcellulose/saline water

      Solubility: 5 mg/mL (9.99 mM); Suspension 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: 99.97%

    SDS (392 KB)

    COA (249 KB) HNMR (287 KB) LCMS (266 KB) Elemental Analysis Report (106 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Total protein is extracted from the cell pellet using a lysis solution containing 50 mM HEPES (pH 7.9), 0.4 mol/L NaCl, and 1 mM EDTA and fortified with 10 µL/mL phosphatase inhibitor cocktail 1, 10 µL/mL phosphatase inhibitor cocktail 2, 10 µL/mL protease inhibitor, and 1% NP-40. Protein concentration of the lysates is determined by the Bio-Rad protein assay. Equal amounts of protein are separated by 12% SDS-PAGE and transferred to an Immobilon membrane. Nonspecific binding sites on the membrane are blocked in 5% nonfat dry milk in Tris (20 mM)-buffered saline (150 mM, pH 7.4) with 0.1% Tween (TBS-T). Protein signals are detected by incubating the membrane in primary antibody in 5% nonfat dry milk overnight at 4°C, followed by a 45-min incubation in the appropriate peroxidase-conjugated secondary antibody. The membrane is then developed by enhanced chemiluminescence with ECL plus Western Blotting Detection Reagents on a Typhoon 9400 scanner.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Tumor xenografts are produced in the leg by im inoculation of 1×106 Calu-6 cells in 10 µL. Irradiation and Adavosertib (MK-1775) treatment are started when tumors reach 8 mm diameter and continue for 5 days. Gamma-rays are delivered locally to the tumor-bearing legs of unanesthetized mice using a small-animal irradiator consisting of two parallel-opposed 137Cs sources, at a dose rate of 5 Gy/min. Tumors are irradiated twice daily separated by 6 h. Adavosertib (MK-1775) is given by gavage in 0.1 mL volumes 1 h before and 2 h after the first daily radiation dose.

    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 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 1.9976 mL 9.9880 mL 19.9760 mL 49.9401 mL
    5 mM 0.3995 mL 1.9976 mL 3.9952 mL 9.9880 mL
    10 mM 0.1998 mL 0.9988 mL 1.9976 mL 4.9940 mL
    15 mM 0.1332 mL 0.6659 mL 1.3317 mL 3.3293 mL
    20 mM 0.0999 mL 0.4994 mL 0.9988 mL 2.4970 mL
    25 mM 0.0799 mL 0.3995 mL 0.7990 mL 1.9976 mL
    30 mM 0.0666 mL 0.3329 mL 0.6659 mL 1.6647 mL
    40 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2485 mL
    50 mM 0.0400 mL 0.1998 mL 0.3995 mL 0.9988 mL
    60 mM 0.0333 mL 0.1665 mL 0.3329 mL 0.8323 mL
    80 mM 0.0250 mL 0.1249 mL 0.2497 mL 0.6243 mL
    100 mM 0.0200 mL 0.0999 mL 0.1998 mL 0.4994 mL
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    Adavosertib 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.

    Keywords:

    Adavosertib955365-80-7AZD1775 MK-1775AZD 1775AZD-1775MK1775MK 1775MK-1775Wee1Inhibitorinhibitorinhibit

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