1. Cell Cycle/DNA Damage
  2. Wee1

MK-1775 (Synonyms: AZD1775)

Cat. No.: HY-10993 Purity: 99.60%
Data Sheet SDS Handling Instructions

MK-1775 is a potent Wee1 inhibitor with IC50 of 5.2 nM.

For research use only. We do not sell to patients.
MK-1775 Chemical Structure

MK-1775 Chemical Structure

CAS No. : 955365-80-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $77 In-stock
5 mg $70 In-stock
10 mg $90 In-stock
50 mg $250 In-stock
100 mg $450 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

    MK-1775 purchased from MCE. Usage Cited in: Alma Mater Studiorum Università di Bologna. 22 Aprile 2016.

    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).

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    MK-1775 is a potent Wee1 inhibitor with IC50 of 5.2 nM.

    IC50 & Target

    IC50: 5.2 nM (Wee1)

    In Vitro

    MK-1775 enhances the cytotoxic effects of 5-FU in p53-deficient human colon cancer cells. 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]. MK-1775 abrogates the radiation-induced G2 block in p53-defective cells but not in p53 wild-type lines[2]. The combination of gemcitabine with MK-1775 produces robust anti-tumor activity and remarkably enhances tumor regression response (4.01 fold) compared to gemcitabine treatment in p53-deficient tumors[3].

    In Vivo

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

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume 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.
    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 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. 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
    Molecular Weight

    500.6

    Formula

    C₂₇H₃₂N₈O₂

    CAS No.

    955365-80-7

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.60%

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    Inquiry Information

    Product Name:
    MK-1775
    Cat. No.:
    HY-10993
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