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

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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

Top Publications Citing Use of Products

    MK-1775 purchased from MCE. Usage Cited in: Cancer Res. 2017 Jun 26. pii: canres.3565.2016.

    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.

    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
    NCT Number Sponsor Condition Start Date Phase
    NCT02482311 AstraZeneca Ovarian Cancer, TNBC, SCLC, Other Solid Tumours July 1, 2015 Phase 1
    NCT02610075 AstraZeneca Locally Advanced Solid Tumours|Metastatic Solid Tumours|Ovarian Cancer December 1, 2015 Phase 1
    NCT01748825 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Neoplasms|Lymphoma November 14, 2012 Phase 1
    NCT02207010 St. Joseph's Hospital and Medical Center, Phoenix|The Ben & Catherine Ivy Foundation|American Society of Clinical Oncology|Barbara Ann Karmanos Cancer Institute|Translational Genomics Research Institute Glioblastoma|GBM July 2014 Early Phase 1
    NCT02511795 AstraZeneca Ovarian, Breast, and Second-Line Small Cell Lung Cancer August 6, 2015 Phase 1
    NCT02593019 Samsung Medical Center Small Cell Lung Cancer December 2015 Phase 2
    NCT02688907 Samsung Medical Center Small Cell Lung Cancer April 2016 Phase 2
    NCT02272790 AstraZeneca Ovarian, Fallopian Tube, Peritoneal Cancer, P53 Mutation January 30, 2015 Phase 2
    NCT02341456 AstraZeneca Advanced Solid Tumours January 16, 2015 Phase 1
    NCT02381548 National Cancer Institute (NCI) Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Previously Treated Myelodysplastic Syndrome|Recurrent Adult Acute Myeloid Leukemia|Refractory Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Secondary Acute Myeloid Leukemia|Therapy-Related Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia August 18, 2015 Phase 1
    NCT02513563 H. Lee Moffitt Cancer Center and Research Institute Lung Cancer September 8, 2015 Phase 2
    NCT02617277 AstraZeneca Advanced Solid Tumours December 28, 2015 Phase 1
    NCT02906059 New York University School of Medicine|AstraZeneca Metastatic Colorectal Cancer September 2016 Phase 1
    NCT02791919 National Cancer Institute (NCI) CNS 2a|CNS 2b|CNS 2c|CNS1|Recurrent Adult Acute Myeloid Leukemia|Recurrent Childhood Acute Myeloid Leukemia May 25, 2017 Phase 1
    NCT01849146 National Cancer Institute (NCI) Adult Glioblastoma|Recurrent Glioblastoma August 19, 2013 Phase 1
    NCT02087176 AstraZeneca Previously Treated Non Small Cell Lung Cancer March 2014 Phase 2
    NCT03012477 Dana-Farber Cancer Institute|AstraZeneca Triple-negative Metastatic Breast Cancer January 18, 2017 Phase 2
    NCT02659241 M.D. Anderson Cancer Center|AstraZeneca Ovarian Cancer|Fallopian Tube Cancer|Peritoneum Cancer February 2016 Early Phase 1
    NCT01922076 National Cancer Institute (NCI) Diffuse Intrinsic Pontine Glioma|Untreated Childhood Anaplastic Astrocytoma|Untreated Childhood Anaplastic Oligoastrocytoma|Untreated Childhood Glioblastoma|Untreated Childhood Gliosarcoma September 3, 2013 Phase 1
    NCT02087241 AstraZeneca Previously Untreated Stage IV Non-Squamous Non Small Cell Lung Cancer March 2014 Phase 2
    NCT02585973 UNC Lineberger Comprehensive Cancer Center|AstraZeneca Carcinoma, Squamous Cell of Head and Neck February 2016 Phase 1
    NCT02666950 Mayo Clinic|National Cancer Institute (NCI) Chronic Myelomonocytic Leukemia|Myelodysplastic Syndrome With Isolated Del(5q)|Myelodysplastic/Myeloproliferative Neoplasm|Previously Treated Myelodysplastic Syndrome|Recurrent Adult Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia May 5, 2017 Phase 2
    NCT02448329 Samsung Medical Center Advanced Gastric Adenocarcinoma January 14, 2015 Phase 2
    NCT01958658 National Cancer Institute (NCI) Stage IB Cervical Cancer|Stage IIA Cervical Cancer|Stage IIB Cervical Cancer|Stage IIIA Cervical Cancer|Stage IIIB Cervical Cancer September 5, 2013 Phase 1
    NCT03028766 University of Birmingham|AstraZeneca|Cancer Research UK Hypopharynx Squamous Cell Carcinoma|Oral Cavity Squamous Cell Carcinoma|Larynx Cancer May 2017 Phase 1
    NCT02508246 University of Washington|National Cancer Institute (NCI) Head and Neck Squamous Cell Carcinoma July 22, 2015 Phase 1
    NCT02095132 National Cancer Institute (NCI) Childhood Central Nervous System Neoplasm|Recurrent Childhood Medulloblastoma|Recurrent Childhood Supratentorial Embryonal Tumor, Not Otherwise Specified|Recurrent Malignant Solid Neoplasm|Recurrent Neuroblastoma March 27, 2014 Phase 1|Phase 2
    NCT02576444 Joseph Paul Eder|Dana-Farber Cancer Institute|Vanderbilt-Ingram Cancer Center|Yale University Cancer November 2015 Phase 2
    NCT02196168 National Cancer Institute (NCI) Recurrent Hypopharyngeal Squamous Cell Carcinoma|Recurrent Laryngeal Squamous Cell Carcinoma|Recurrent Laryngeal Verrucous Carcinoma|Recurrent Lip and Oral Cavity Squamous Cell Carcinoma|Recurrent Metastatic Squamous Cell Carcinoma in the Neck With Occult Primary|Recurrent Nasal Cavity and Paranasal Sinus Squamous Cell Carcinoma|Recurrent Oral Cavity Verrucous Carcinoma|Recurrent Oropharyngeal Squamous Cell Carcinoma|Squamous Cell Carcinoma Metastatic in the Neck With Occult Primary|Stage IV Hyp March 2014 Phase 2
    NCT02194829 National Cancer Institute (NCI) Metastatic Pancreatic Adenocarcinoma|Stage III Pancreatic Cancer AJCC v6 and v7|Stage IV Pancreatic Cancer AJCC v6 and v7|Unresectable Pancreatic Carcinoma July 1, 2014 Phase 1|Phase 2
    NCT02937818 AstraZeneca Platinum Refractory Extensive-Stage Small Cell Lung Carcinoma November 28, 2016 Phase 2
    NCT02101775 National Cancer Institute (NCI) Ovarian Brenner Tumor|Ovarian Carcinosarcoma|Ovarian Clear Cell Cystadenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Cystadenocarcinoma|Ovarian Seromucinous Carcinoma|Ovarian Serous Cystadenocarcinoma|Ovarian Serous Surface Papillary Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Ovarian Carcinoma July 21, 2014 Phase 2
    NCT02546661 AstraZeneca Muscle Invasive Bladder Cancer October 3, 2016 Phase 1
    NCT02465060 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|Bladder Carcinoma|Breast Carcinoma|Cervical Carcinoma|Colon Carcinoma|Colorectal Carcinoma|Endometrial Carcinoma|Esophageal Carcinoma|Gastric Carcinoma|Glioma|Head and Neck Carcinoma|Kidney Carcinoma|Liver and Intrahepatic Bile Duct Carcinoma|Lung Carcinoma|Lymphoma|Malignant Uterine Neoplasm|Melanoma|Ovarian Carcinoma|Pancreatic Carcinoma|Plasma Cell Myeloma|Prostate Carcinoma|Rectal Carcinoma|Recurrent Bladder Carcinoma|Recurrent Breast Carcinoma|Recurrent Cer August 12, 2015 Phase 2
    NCT02813135 Gustave Roussy, Cancer Campus, Grand Paris|National Cancer Institute, France Children, Adolescents and Young Adults With Refractory or Recurrent Malignancies June 2016 Phase 1|Phase 2
    NCT01827384 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|Recurrent Malignant Solid Neoplasm December 31, 2013 Phase 2
    NCT02482311 AstraZeneca Ovarian Cancer, TNBC, SCLC, Other Solid Tumours July 1, 2015 Phase 1
    NCT02610075 AstraZeneca Locally Advanced Solid Tumours|Metastatic Solid Tumours|Ovarian Cancer December 1, 2015 Phase 1
    NCT01748825 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Neoplasms|Lymphoma November 14, 2012 Phase 1
    NCT02207010 St. Joseph's Hospital and Medical Center, Phoenix|The Ben & Catherine Ivy Foundation|American Society of Clinical Oncology|Barbara Ann Karmanos Cancer Institute|Translational Genomics Research Institute Glioblastoma|GBM July 2014 Early Phase 1
    NCT02511795 AstraZeneca Ovarian, Breast, and Second-Line Small Cell Lung Cancer August 6, 2015 Phase 1
    NCT02593019 Samsung Medical Center Small Cell Lung Cancer December 2015 Phase 2
    NCT02688907 Samsung Medical Center Small Cell Lung Cancer April 2016 Phase 2
    NCT02272790 AstraZeneca Ovarian, Fallopian Tube, Peritoneal Cancer, P53 Mutation January 30, 2015 Phase 2
    NCT02341456 AstraZeneca Advanced Solid Tumours January 16, 2015 Phase 1
    NCT02381548 National Cancer Institute (NCI) Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Previously Treated Myelodysplastic Syndrome|Recurrent Adult Acute Myeloid Leukemia|Refractory Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Secondary Acute Myeloid Leukemia|Therapy-Related Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia August 18, 2015 Phase 1
    NCT02513563 H. Lee Moffitt Cancer Center and Research Institute Lung Cancer September 8, 2015 Phase 2
    NCT02617277 AstraZeneca Advanced Solid Tumours December 28, 2015 Phase 1
    NCT02906059 New York University School of Medicine|AstraZeneca Metastatic Colorectal Cancer September 2016 Phase 1
    NCT02791919 National Cancer Institute (NCI) CNS 2a|CNS 2b|CNS 2c|CNS1|Recurrent Adult Acute Myeloid Leukemia|Recurrent Childhood Acute Myeloid Leukemia May 25, 2017 Phase 1
    NCT01849146 National Cancer Institute (NCI) Adult Glioblastoma|Recurrent Glioblastoma August 19, 2013 Phase 1
    NCT02087176 AstraZeneca Previously Treated Non Small Cell Lung Cancer March 2014 Phase 2
    NCT03012477 Dana-Farber Cancer Institute|AstraZeneca Triple-negative Metastatic Breast Cancer January 18, 2017 Phase 2
    NCT02659241 M.D. Anderson Cancer Center|AstraZeneca Ovarian Cancer|Fallopian Tube Cancer|Peritoneum Cancer February 2016 Early Phase 1
    NCT01922076 National Cancer Institute (NCI) Diffuse Intrinsic Pontine Glioma|Untreated Childhood Anaplastic Astrocytoma|Untreated Childhood Anaplastic Oligoastrocytoma|Untreated Childhood Glioblastoma|Untreated Childhood Gliosarcoma September 3, 2013 Phase 1
    NCT02087241 AstraZeneca Previously Untreated Stage IV Non-Squamous Non Small Cell Lung Cancer March 2014 Phase 2
    NCT02585973 UNC Lineberger Comprehensive Cancer Center|AstraZeneca Carcinoma, Squamous Cell of Head and Neck February 2016 Phase 1
    NCT02666950 Mayo Clinic|National Cancer Institute (NCI) Chronic Myelomonocytic Leukemia|Myelodysplastic Syndrome With Isolated Del(5q)|Myelodysplastic/Myeloproliferative Neoplasm|Previously Treated Myelodysplastic Syndrome|Recurrent Adult Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia May 5, 2017 Phase 2
    NCT02448329 Samsung Medical Center Advanced Gastric Adenocarcinoma January 14, 2015 Phase 2
    NCT01958658 National Cancer Institute (NCI) Stage IB Cervical Cancer|Stage IIA Cervical Cancer|Stage IIB Cervical Cancer|Stage IIIA Cervical Cancer|Stage IIIB Cervical Cancer September 5, 2013 Phase 1
    NCT03028766 University of Birmingham|AstraZeneca|Cancer Research UK Hypopharynx Squamous Cell Carcinoma|Oral Cavity Squamous Cell Carcinoma|Larynx Cancer May 2017 Phase 1
    NCT02508246 University of Washington|National Cancer Institute (NCI) Head and Neck Squamous Cell Carcinoma July 22, 2015 Phase 1
    NCT02095132 National Cancer Institute (NCI) Childhood Central Nervous System Neoplasm|Recurrent Childhood Medulloblastoma|Recurrent Childhood Supratentorial Embryonal Tumor, Not Otherwise Specified|Recurrent Malignant Solid Neoplasm|Recurrent Neuroblastoma March 27, 2014 Phase 1|Phase 2
    NCT02576444 Joseph Paul Eder|Dana-Farber Cancer Institute|Vanderbilt-Ingram Cancer Center|Yale University Cancer November 2015 Phase 2
    NCT02196168 National Cancer Institute (NCI) Recurrent Hypopharyngeal Squamous Cell Carcinoma|Recurrent Laryngeal Squamous Cell Carcinoma|Recurrent Laryngeal Verrucous Carcinoma|Recurrent Lip and Oral Cavity Squamous Cell Carcinoma|Recurrent Metastatic Squamous Cell Carcinoma in the Neck With Occult Primary|Recurrent Nasal Cavity and Paranasal Sinus Squamous Cell Carcinoma|Recurrent Oral Cavity Verrucous Carcinoma|Recurrent Oropharyngeal Squamous Cell Carcinoma|Squamous Cell Carcinoma Metastatic in the Neck With Occult Primary|Stage IV Hyp March 2014 Phase 2
    NCT02194829 National Cancer Institute (NCI) Metastatic Pancreatic Adenocarcinoma|Stage III Pancreatic Cancer AJCC v6 and v7|Stage IV Pancreatic Cancer AJCC v6 and v7|Unresectable Pancreatic Carcinoma July 1, 2014 Phase 1|Phase 2
    NCT02937818 AstraZeneca Platinum Refractory Extensive-Stage Small Cell Lung Carcinoma November 28, 2016 Phase 2
    NCT02101775 National Cancer Institute (NCI) Ovarian Brenner Tumor|Ovarian Carcinosarcoma|Ovarian Clear Cell Cystadenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Cystadenocarcinoma|Ovarian Seromucinous Carcinoma|Ovarian Serous Cystadenocarcinoma|Ovarian Serous Surface Papillary Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Ovarian Carcinoma July 21, 2014 Phase 2
    NCT02546661 AstraZeneca Muscle Invasive Bladder Cancer October 3, 2016 Phase 1
    NCT02465060 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|Bladder Carcinoma|Breast Carcinoma|Cervical Carcinoma|Colon Carcinoma|Colorectal Carcinoma|Endometrial Carcinoma|Esophageal Carcinoma|Gastric Carcinoma|Glioma|Head and Neck Carcinoma|Kidney Carcinoma|Liver and Intrahepatic Bile Duct Carcinoma|Lung Carcinoma|Lymphoma|Malignant Uterine Neoplasm|Melanoma|Ovarian Carcinoma|Pancreatic Carcinoma|Plasma Cell Myeloma|Prostate Carcinoma|Rectal Carcinoma|Recurrent Bladder Carcinoma|Recurrent Breast Carcinoma|Recurrent Cer August 12, 2015 Phase 2
    NCT02813135 Gustave Roussy, Cancer Campus, Grand Paris|National Cancer Institute, France Children, Adolescents and Young Adults With Refractory or Recurrent Malignancies June 2016 Phase 1|Phase 2
    NCT01827384 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|Recurrent Malignant Solid Neoplasm December 31, 2013 Phase 2
    NCT01164995 The Netherlands Cancer Institute|Merck Sharp & Dohme Corp. Epithelial Ovarian Cancer July 2010 Phase 2
    NCT01357161 Merck Sharp & Dohme Corp. Ovarian Cancer July 2011 Phase 2
    NCT02037230 University of Michigan Cancer Center Adenocarcinoma of the Pancreas January 2014 Phase 1|Phase 2
    View MoreCollapse
    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) 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
    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
    M.Wt

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