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Alisertib

MLN8237,MLN 8237,MLN-8237

Alisertib (MLN8237)是一种选择性的Aurora A抑制剂，IC50为1.2 nM，作用于Aurora A比作用于Aurora B选择性强200倍以上。

目录号
EY1556
EY1556
EY1556
EY1556
纯度
98.98%
98.98%
98.98%
98.98%
规格
5 mg
10 mg
50 mg
100 mg
原价
676
972
2820
3710
售价
676
972
2820
3710
库存
现货
现货
现货
现货
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  • 生物活性

    The orally bioavailable agent, MLN8237 (also known as alisertib), is a potent small-molecule inhibitor of Aurora A kinase (AAK) which is overexpressed in several types of tumor and associated with oncogenesis and tumor progression. It was developed from its predecessor, MLN8054, in order to minimize the benzodiazepine-like effects seen with MLN8054. The inhibitory effect of MLN8237 is ATP-competitive, reversible and AAK-specific with an inhibition constant (Ki) of 0.43 nmol/L. MLN8237 is being investigated to treat advanced malignancies, due to its both in vitro and in vivo activities against a broad range of tumor types.

  • 体外研究

  • 体内研究

    15% Captisol

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    ~30 mg/kg/day 口服处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Manfredi MG, et al. Clin Cancer Res, 2011, 17(24), 7614-7624.

    分子式
    C27H20ClFN4O4    		 分子量
    518.92    		 CAS号
    1028486-01-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    30 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02214147 Advanced Solid Tumors|Relapsed/Refractory Lymphoma Drug: Alisertib Millennium Pharmaceuticals, Inc.|Takeda Phase 1 2014-09-01 2016-08-26
    NCT01898078 Advanced Solid Tumors|Lymphoma Drug: MLN8237 Millennium Pharmaceuticals, Inc.|Takeda Phase 1 2013-07-01 2017-01-31
    NCT02812056 Malignant Neoplasms of Digestive Organs|Malignant Neoplasms of Female Genital Organs|Malignant Neoplasms of Lip Oral Cavity and Pharynx|Malignant Neoplasms of Male Genital Organs Drug: Alisertib|Drug: TAK-228 M.D. Anderson Cancer Center|Millennium Pharmaceuticals, Inc. Phase 1 2016-09-01 2017-03-24
    NCT02719691 Metastatic Breast Cancer|Solid Tumors Drug: Alisertib|Drug: MLN0128 University of Colorado, Denver Phase 1 2016-05-01 2016-11-07
    NCT01512758 Advanced Solid Tumors|Lymphomas Drug: Alisertib Millennium Pharmaceuticals, Inc. Phase 1 2012-02-01 2015-10-15
    NCT01714947 Advanced Solid Tumors|Lymphoma Drug: alisertib Millennium Pharmaceuticals, Inc. Phase 1 2013-01-01 2013-09-03
    NCT02293005 Lung Cancer|Mesothelioma Drug: Alisertib M.D. Anderson Cancer Center|Millennium Pharmaceuticals, Inc. Phase 2 2015-05-20 2017-02-15
    NCT02700022 Diffuse Large B-cell Lymphoma|Follicular Lymphoma|Burkitt Lymphoma Drug: Alisertib UNC Lineberger Comprehensive Cancer Center|Millennium Pharmaceuticals, Inc. Phase 1 2016-07-01 2017-03-17
    NCT02109328 Bladder Cancer|Transitional Cell Carcinoma Drug: Alisertib|Drug: Paclitaxel|Drug: Placebo Fondazione IRCCS Istituto Nazionale dei Tumori, Milano Phase 2 2014-04-01 2014-04-07
    NCT02186509 Adult Anaplastic Astrocytoma|Adult Anaplastic Ependymoma|Adult Anaplastic Oligodendroglioma|Adult Brain Stem Glioma|Adult Diffuse Astrocytoma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Adult Oligodendroglioma|Adult Pilocytic Astrocytoma|Adult Pineal Gland Astrocytoma|Adult Subependymal Giant Cell Astrocytoma|Recurrent Adult Brain Tumor Radiation: Hyperfractionated radiation therapy|Radiation: Stereotactic radiosurgery|Drug: Alisertib|Procedure: Quality-of-life assessment Sidney Kimmel Cancer Center at Thomas Jefferson University|Millennium Pharmaceuticals, Inc.|Thomas Jefferson University Phase 1 2015-01-01 2016-10-19
    NCT01844583 Solid Tumors|Lymphoma Drug: alisertib|Drug: esomeprazole|Drug: rifampin Millennium Pharmaceuticals, Inc.|Takeda Phase 1 2013-07-01 2016-09-29
    NCT02259010 Advanced Solid Tumors|Relapsed/Refractory Lymphoma Drug: Alisertib|Drug: Itraconazole Millennium Pharmaceuticals, Inc. Phase 1 2014-10-01 2016-01-06
    NCT01812005 Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Splenic Marginal Zone Lymphoma|Waldenstr枚m Macroglobulinemia Drug: alisertib|Biological: rituximab|Other: laboratory biomarker analysis Kristie Blum|Millennium Pharmaceuticals, Inc.|Ohio State University Comprehensive Cancer Center Phase 2 2013-05-01 2017-01-11
    NCT01613261 Advanced Nonhematologic Malignancies Drug: TAK-733 and alisertib Millennium Pharmaceuticals, Inc. Phase 1 2013-08-01 2013-10-31
    NCT02219789 Estrogen Receptor Positive|Progesterone Receptor Positive|Recurrent Breast Carcinoma|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Drug: Alisertib|Drug: Fulvestrant|Other: Laboratory Biomarker Analysis Mayo Clinic|National Cancer Institute (NCI) Phase 1 2014-09-01 2016-03-30
    NCT01567709 Adult B Acute Lymphoblastic Leukemia|Adult T Acute Lymphoblastic Leukemia|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-Cell Lymphoma|Chronic Lymphocytic Leukemia|Cutaneous B-Cell Non-Hodgkin Lymphoma|Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue|Hepatosplenic T-Cell Lymphoma|Intraocular Lymphoma|Lymphomatous Involvement of Non-Cutaneous Extranodal Site|Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma|Nodal Marginal Zone Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult Immunoblastic Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Adult T-Cell Leukemia/Lymphoma|Recurrent Cutaneous T-Cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides and Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Hairy Cell Leukemia|Small Intestinal Lymphoma|Splenic Marginal Zone Lymphoma|T-Cell Large Granular Lymphocyte Leukemia|Testicular Lymphoma|Waldenstrom Macroglobulinemia Drug: Alisertib|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Vorinostat National Cancer Institute (NCI) Phase 1 2012-04-01 2016-12-26
    NCT01848067 Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer Drug: Alisertib|Drug: Abiraterone acetate|Drug: Prednisone Sidney Kimmel Cancer Center at Thomas Jefferson University|Millennium: The Takeda Oncology Company|Thomas Jefferson University Phase 1|Phase 2 2013-08-01 2016-10-18
    NCT01779843 Acute Myelogenous Leukemia Drug: Cytarabine|Drug: Idarubicin|Drug: Alisertib Massachusetts General Hospital Phase 1 2013-04-01 2017-02-15
    NCT02187991 Breast Cancer|Breast Carcinoma|Breast Tumors|Malignant Neoplasm of Breast Drug: Paclitaxel|Drug: Alisertib US Oncology Research|Millennium Pharmaceuticals, Inc. Phase 2 2015-02-01 2016-09-15
    NCT01653028 Myxofibrosarcoma|Recurrent Adult Soft Tissue Sarcoma|Recurrent Leiomyosarcoma|Recurrent Liposarcoma|Recurrent Malignant Peripheral Nerve Sheath Tumor|Recurrent Undifferentiated Pleomorphic Sarcoma|Stage III Soft Tissue Sarcoma|Stage IV Soft Tissue Sarcoma Drug: Alisertib|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 2 2012-08-01 2016-11-01
    NCT01799278 Small Cell Prostate Cancer|Neuroendocrine Prostate Cancer|Prostate Adenocarcinoma Plus > 50% Immunohistochemical Staining for Neuroendocrine Markers Drug: MLN8237 Weill Medical College of Cornell University|Millennium Pharmaceuticals, Inc. Phase 2 2013-02-01 2017-01-19

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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