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Saracatinib

塞卡替尼,AZD0530

Saracatinib (AZD0530)是一种有效的Src抑制剂，IC50为2.7 nM，对c-Yes， Fyn， Lyn， Blk， Fgr和Lck等也有活性；但对Abl和EGFR (L858R和L861Q)活性较低。

目录号
EY1111
EY1111
EY1111
EY1111
EY1111
纯度
99.68%
99.68%
99.68%
99.68%
99.68%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
145
290
502
1210
2400
售价
145
290
502
1210
2400
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
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  • 生物活性

    Saracatinib has been reported to inhibit Src activation in DU145 and PC3 cell lines (prostate cancer cell lines). Both of c-Myc and cyclin D1 expression are decreased by Saracatinib. Saracatinib can inhibit the ERK1/2 and GSK3b phosphorylation as well as decrease β-catenin level in cells. Saracatinib inhibits the prostate tumor cell growth by inducing cycle arrest at G1/S phase. Saracatinib dose-dependently blocks cell migration in DU145 and PC3 cell lines.

  • 体外研究

  • 体内研究

    0.5% methylcellulose+0.2% Tween 80

  • 激酶实验

  • 细胞实验

    62.5 nM-16 mM

  • 动物实验

    25 mg/kg 每天口服处理

  • 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] Chang YM, Oncogene, 2008, 27(49), 6365-6375.
    [2] Purnell PR, et al. The Src inhibitor AZD0530 blocks invasion and may act as a radiosensitizer in lung cancer cells. J Thorac Oncol, 2009, 4(4), 448-454.
    [3] Green TP, et al. Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol Oncol, 2009, 3(3), 248-261.

    分子式
    C27H32ClN5O5    		 分子量
    542.03    		 CAS号
    379231-04-6    		 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
    >30 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
    NCT02116712 Pulmonary Lymphangioleiomyomatosis Drug: Saracatinib Tony Eissa|University of Texas|University of Cincinnati|Baylor College of Medicine Phase 1 2014-08-01 2016-11-28
    NCT02737202 Pulmonary Lymphangioleiomyomatosis Drug: saracatinib Baylor College of Medicine|University of Cincinnati|Brigham and Women's Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) Phase 2 2016-04-01 2016-11-28
    NCT00669019 Recurrent Melanoma|Stage IIA Melanoma|Stage IIB Melanoma|Stage IIC Melanoma|Stage IV Melanoma Drug: saracatinib National Cancer Institute (NCI) Phase 2 2006-07-01 2014-05-06
    NCT02732587 Alcohol Drinking Drug: Saracatinib Yale University|National Institute on Alcohol Abuse and Alcoholism (NIAAA) Phase 1 2015-11-01 2016-04-04
    NCT00607594 Adenocarcinoma of the Gastroesophageal Junction|Adenocarcinoma of the Stomach|Recurrent Gastric Cancer|Stage III Gastric Cancer|Stage III Esophageal Cancer|Stage IV Esophageal Cancer|Stage IV Gastric Cancer Drug: saracatinib National Cancer Institute (NCI) Phase 2 2008-01-01 2014-06-19
    NCT01864655 Alzheimer's Disease Drug: saracatinib|Drug: Placebo Stephen M. Strittmatter|Yale University Phase 1 2013-07-01 2014-06-12
    NCT00638937 Recurrent Non-small Cell Lung Cancer|Stage IIIB Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer Drug: saracatinib National Cancer Institute (NCI) Phase 2 2008-02-01 2015-06-22
    NCT00718809 Invasive Thymoma and Thymic Carcinoma|Recurrent Thymoma and Thymic Carcinoma|Stage III Thymoma|Stage IVA Thymoma|Stage IVB Thymoma Drug: saracatinib National Cancer Institute (NCI) Phase 2 2008-06-01 2015-06-05
    NCT00528645 Extensive Stage Small Cell Lung Cancer|Lung Metastases|Malignant Pleural Effusion|Recurrent Small Cell Lung Cancer Drug: saracatinib National Cancer Institute (NCI) Phase 2 2007-11-01 2014-05-29
    NCT02955186 Alcohol Drinking Drug: Saracatinib|Drug: Placebos Yale University Phase 2 2017-01-01 2016-11-03
    NCT01267266 Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer Drug: saracatinib|Other: hydrocortisone/placebo National Cancer Institute (NCI) Phase 2 2010-12-01 2015-03-18
    NCT02085603 Cancer Drug: Saracatinib|Drug: Placebo Sheffield Teaching Hospitals NHS Foundation Trust|AstraZeneca Phase 2 2014-03-01 2014-11-11
    NCT00559507 Estrogen Receptor-negative Breast Cancer|Male Breast Cancer|Progesterone Receptor-negative Breast Cancer|Recurrent Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Drug: saracatinib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2007-10-01 2014-04-02
    NCT00397878 Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum|Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IV Colon Cancer|Stage IV Rectal Cancer Drug: saracatinib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2006-11-01 2014-05-07
    NCT00513071 Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer Drug: saracatinib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2007-08-01 2014-10-01
    NCT00659360 Adult Fibrosarcoma|Adult Leiomyosarcoma|Adult Liposarcoma|Adult Malignant Fibrous Histiocytoma|Adult Rhabdomyosarcoma|Dermatofibrosarcoma Protuberans|Endometrial Stromal Sarcoma|Recurrent Adult Soft Tissue Sarcoma|Recurrent Uterine Sarcoma|Stage III Adult Soft Tissue Sarcoma|Stage III Uterine Sarcoma|Stage IV Adult Soft Tissue Sarcoma|Stage IV Uterine Sarcoma|Uterine Carcinosarcoma|Uterine Leiomyosarcoma Drug: saracatinib National Cancer Institute (NCI) Phase 2 2008-02-01 2015-07-02
    NCT00752206 Osteosarcoma Drug: Saracatinib|Drug: Placebo Sarcoma Alliance for Research through Collaboration|AstraZeneca Phase 2 2009-03-01 2017-03-20
    NCT02262026 Alcoholism Drug: 125 mg AZD0530|Drug: 50 mg AZD0530|Drug: Placebo Yale University Phase 1 2014-11-01 2016-11-18
    NCT00558272 Breast Cancer|Prostate Cancer|Bone Neoplasms Drug: AZD0530|Drug: Zoledronic Acid AstraZeneca Phase 2 2008-02-01 2013-05-23
    NCT01196741 Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer Drug: Paclitaxel|Drug: Saracatinib|Drug: Matched placebo University College, London|AstraZeneca|Cancer Research UK Phase 2|Phase 3 2011-03-01 2015-04-17
    NCT02167256 Alzheimer's Disease Drug: AZD0530 100mg daily|Drug: AZD0530 125mg daily|Drug: Placebo Yale University|Alzheimer's Therapeutic Research Institute Phase 2 2014-12-01 2016-12-01
    NCT00704366 Solid Tumor Drug: AZD0530 AstraZeneca Phase 1 2008-06-01 2011-05-13
    NCT00771979 Healthy Drug: AZD0530|Drug: AZD0530 AstraZeneca Phase 1 2008-11-01 2009-06-17
    NCT00475956 Neoplasms Drug: AZD2171|Drug: AZD0530 AstraZeneca Phase 1 2007-05-01 2010-04-14

    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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