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

Adavosertib (Synonyms: AZD1775; MK-1775)

Cat. No.: HY-10993 Purity: 99.96%
Handling Instructions

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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10 mM * 1 mL in DMSO USD 55 In-stock
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10 mg USD 80 In-stock
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50 mg USD 150 In-stock
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100 mg USD 250 In-stock
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Customer Review

Based on 12 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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 MCE. 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).

    Adavosertib purchased from MCE. Usage Cited in: J Hematol Oncol. 2018 Aug 1;11(1):99.

    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.
    • Biological Activity

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    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)

    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].

    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].

    Clinical Trial
    Molecular Weight

    500.60

    Formula

    C₂₇H₃₂N₈O₂

    CAS No.

    955365-80-7

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 18.75 mg/mL (37.46 mM; Need ultrasonic)

    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
    10 mM 0.1998 mL 0.9988 mL 1.9976 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      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

    • 2.

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

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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.96%

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    Adavosertib
    Cat. No.:
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