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Dovitinib

多韦替尼,多维替尼,TKI-258,CHIR-258

Dovitinib是多靶点RTK抑制剂，对FLT3和c-Kit的IC50分别为1 nM和2 nM，对FGFR1/3和VEGFR1-4的IC50为8-13 nM，对InsR，EGFR，c-Met，EphA2，Tie2和Dovitinib(CHIR-258; TKI258)是多靶点RTK抑制剂，对FLT3和c-Kit的IC50分别为1 nM和2 nM，对FGFR1/3和VEGFR1-4的IC50为8-13 nM，对InsR，EGFR，c-Met，EphA2，Tie2和IGFR抑制性较弱。

目录号
EY1549
EY1549
EY1549
纯度
99.28%
99.28%
99.28%
规格
1 mg
5 mg
10 mg
原价
150
400
700
售价
150
400
700
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    400 nM 左右

  • 动物实验

    10, 30,或60 mg/kg饲喂处理

  • 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] Trudel, Suzanne., et al., 2005. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 105(7): 2941-8.

    分子式
    C21H21FN6O    		 分子量
    392.43    		 CAS号
    405169-16-6    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    10 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
    NCT01478373 Gastrointestinal Stromal Tumors Drug: Dovitinib (TKI258) Novartis Pharmaceuticals|Novartis Phase 2 2012-01-01 2016-04-26
    NCT01417143 Adenoid Cystic Carcinoma Drug: TKI258 (Dovitinib): Seoul National University Hospital Phase 2 2011-09-01 2014-11-11
    NCT01732107 Bladder Cancer Drug: Dovitinib Noah Hahn, M.D.|Novartis Pharmaceuticals|Hoosier Cancer Research Network Phase 2 2013-03-01 2017-03-07
    NCT01791387 Clear Cell Renal Cell Carcinoma Drug: Dovitinib Auckland District Health Board|University of Auckland, New Zealand|IGENZ, Ltd., Auckland|Novartis Phase 2 2012-03-01 2015-02-01
    NCT01831726 Tumor Pathway Activations Inhibited by Dovitinib Drug: Dovitinib (TKI258) Novartis Pharmaceuticals|Novartis Phase 2 2013-08-01 2017-01-30
    NCT01714765 Metastatic Clear Cell Renal Cancer Drug: Dovitinib|Drug: Everolimus Queen Mary University of London|Novartis Phase 1 2011-04-01 2013-11-11
    NCT01921673 Gastric Cancer Drug: Dovitinib and docetaxel Asan Medical Center|Novartis Pharmaceuticals Phase 1|Phase 2 2013-08-01 2015-11-26
    NCT01514526 Adrenocortical Carcinoma Drug: Dovitinib Spanish Oncology Genito-Urinary Group Phase 2 2012-01-01 2016-04-14
    NCT01888965 Colorectal Cancer|Pancreas Cancer Drug: Dovitinib Georgetown University|Novartis Phase 2 2013-10-01 2016-06-07
    NCT02268435 Gastrointestinal Stromal Tumors Drug: dovitinib plus imatinib Asan Medical Center Phase 1 2015-03-01 2015-08-01
    NCT01676714 Non-Small Cell Lung Cancer|Colorectal Cancer Drug: Dovitinib University of California, Davis|Novartis Phase 2 2013-02-01 2016-06-20
    NCT01678105 Recurrent Adenoid Cystic Carcinoma of the Salivary Glands|Metastatic Adenoid Cystic Carcinoma of the Salivary Glands|Salivary Gland Cancers|ACC Drug: Dovitinib Ontario Clinical Oncology Group (OCOG)|Novartis Pharmaceuticals Phase 2 2012-11-01 2015-09-16
    NCT01484041 Breast Cancer Drug: Dovitinib|Drug: Aromatase Inhibitors Georgetown University|Novartis Pharmaceuticals Phase 1|Phase 2 2012-04-01 2017-01-16
    NCT01769547 Advanced Malignant Pleural Mesothelioma|MPM Drug: Dovitinib Ontario Clinical Oncology Group (OCOG)|Novartis Pharmaceuticals Phase 2 2013-03-01 2015-09-16
    NCT01223027 Metastatic Renal Cell Carcinoma Drug: Dovitinib|Drug: Sorafenib Novartis Pharmaceuticals|Novartis Phase 3 2011-03-01 2015-11-05
    NCT01680796 Multiple Myeloma Drug: Dovitinib|Drug: Bortezomib|Drug: Dexamethasone University of Florida|Novartis Pharmaceuticals Phase 1 2013-02-01 2013-02-18
    NCT01700270 Advanced Solid Tumors, Excluding Breast Cancer Drug: dovitinib (TKI258)|Drug: fluvoxamine Novartis Pharmaceuticals|Novartis Phase 1 2013-05-01 2014-11-04
    NCT02065323 Prostate Cancer Drug: Standard ADT|Drug: Dovitinib Oscar Goodman, Jr.|Comprehensive Cancer Centers of Nevada Phase 2 null 2015-01-15
    NCT01964144 Thyroid Cancer Drug: Dovitinib Yonsei University Phase 2 2013-01-01 2014-11-26
    NCT01262027 Breast Cancer Drug: Dovitinib M.D. Anderson Cancer Center|Novartis Phase 2 2012-01-01 2016-12-08

    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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