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Bosutinib

博舒替尼,泊舒替尼,博苏替尼,SKI-606,SKI606,SKI 606

Bosutinib (SKI-606)是一种新型的Sarcoma/Abelson (Src/Abl)酪氨酸激酶双重抑制剂，其IC50分别为1.2 nM和1 nM。

目录号
EY1727
EY1727
EY1727
EY1727
纯度
99.26%
99.26%
99.26%
99.26%
规格
5 mg
10 mg
50 mg
100 mg
原价
270
440
830
1060
售价
270
440
830
1060
库存
现货
现货
现货
现货
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订购
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  • 生物活性

    In chronic myelogenous leukemia (CML) cells, SKI-606 inhibited phosphorylation of Bcr-Abl, Src and Stat5. It also ablated the expression of v-Abl in fibroblasts and blocked proliferation of CML cells. In colorectal cancer cells, SKI-606 inhibited Src autophosphorylation with an IC50 of ~ 0.25 μM, and simultaneity suppressed Tyr (925) phosphorylation of a Src substrate. SKI-606 blocked beta-catenin function by inhibiting its binding to the TCF4 transcription factor and dose-dependently suppressed cyclin D1. SKI-606 increased its binding affinity of beta-catenin to E-cadherin and adhesion, with ensuing reduced motility in a wound healing assay.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    1 μM

  • 动物实验

    150 mg/kg/day 口服饲喂

  • 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] Boschelli DH, et al. J Med Chem, 2001, 44(23), 3965-3977.
    [2] Golas et al (2005) SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res. 65 5358.
    [3] Vultur et al (2008) SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells. Mol.Cancer.Ther. 7 1185.
    [4] Konig, H., et al. 2008. Blood. 111: 2329-2338.

    分子式
    C26H29Cl2N5O3    		 分子量
    530.45    		 CAS号
    380843-75-4    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    ≥15 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    25 mM

    体内溶解度

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

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02906696 Chronic Myelogenous Leukemia Drug: Bosutinib|Behavioral: Phone Calls|Behavioral: Questionnaires M.D. Anderson Cancer Center|Pfizer Phase 2 2016-10-01 2017-03-01
    NCT02546375 Chronic Myeloid Leukaemia Drug: Bosutinib Pfizer|pH Associates 2015-07-01 2017-03-05
    NCT01331291 Glioblastoma Drug: bosutinib Massachusetts General Hospital|Dana-Farber Cancer Institute|Brigham and Women's Hospital|Pfizer Phase 2 2011-04-01 2016-06-23
    NCT02311998 Leukemia Drug: Bosutinib|Drug: Inotuzumab Ozogamicin|Behavioral: Phone Call M.D. Anderson Cancer Center|Pfizer Phase 1|Phase 2 2015-04-01 2017-02-16
    NCT02810990 Chronic Myeloid Leukemia Drug: Bosutinib Gruppo Italiano Malattie EMatologiche dell'Adulto Phase 2 2016-11-01 2016-11-21
    NCT03023319 Carcinoma, Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer Drug: Bosutinib|Drug: Pemetrexed Nagla Karim|University of Cincinnati Phase 1 2017-01-01 2017-01-13
    NCT02782403 Leukemia Drug: Axitinib|Drug: Bosutinib M.D. Anderson Cancer Center|Pfizer Phase 1|Phase 2 2017-03-20 2017-03-20
    NCT02445742 Chronic Myeloblastic Leukaemia Drug: Bosutinib PETHEMA Foundation Phase 2 2015-05-01 2017-01-11
    NCT02130557 Leukemia, Myelogenous, Chronic, Breakpoint Cluster Region-Abelson Proto-oncogene (BCR-ABL) Positive Drug: Bosutinib|Drug: Imatinib Avillion Development 1 Limited Phase 3 2014-06-01 2015-09-16
    NCT01374139 Philadelphia Chromosome Positive (Ph+) Chronic Myeloid Leukemia (CML) Drug: Bosutinib|Drug: Bosutinib Pfizer Phase 1 2011-08-01 2011-11-28
    NCT02501330 Chronic Myelogenous Leukemia Drug: Bosutinib Pfizer 2015-07-01 2017-03-22
    NCT01903733 Chronic Myeloid Leukemia Drug: bosutinib Pfizer 2013-08-28 2017-03-14
    NCT01025570 Pancreatic Cancer Drug: Gemcitabine, Bosutinib University of California, San Francisco|University of Utah Phase 1 2010-05-01 2014-05-07
    NCT00261846 Chronic Myeloid Leukemia Drug: Bosutinib Pfizer Phase 1|Phase 2 2006-03-01 2015-10-27
    NCT00574873 Chronic Myeloid Leukemia Drug: Bosutinib|Drug: imatinib Pfizer|Wyeth is now a wholly owned subsidiary of Pfizer Phase 3 2008-02-01 2016-08-22
    NCT02192294 Healthy Drug: Oral Bosutinib|Drug: Intravenous infusion of bosutinib Pfizer Phase 1 2014-08-01 2014-10-30
    NCT00934674 Healthy Drug: SKI-606 (Bosutinib) Wyeth is now a wholly owned subsidiary of Pfizer Phase 1 2009-07-01 2009-09-01
    NCT00959946 Advanced Breast Cancer (Parts 1 and 2)|Advanced Pancreatic Cancer (Part 1)|Advanced Colorectal Cancer (Part 1)|Advanced Cholangiocarcinoma (Part 1)|Advanced Glioblastoma Multiforme (Part 1) Drug: Bosutinib|Drug: Capecitabine Pfizer Phase 1|Phase 2 2009-09-01 2013-01-18
    NCT00721474 Healthy Subjects Drug: Bosutinib|Drug: Bosutinib Wyeth is now a wholly owned subsidiary of Pfizer Phase 1 2008-09-01 2009-02-05
    NCT02228382 Previously Treated PH + CML Drug: Bosutinib Pfizer|Developmental Therapeutics Consortium Phase 4 2014-11-07 2017-03-14
    NCT01080365 Healthy Drug: SKI-606 (Bosutinib)|Drug: SKI-606 (Bosutinib) Wyeth is now a wholly owned subsidiary of Pfizer Phase 1 2010-02-01 2010-09-03

    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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