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Ponatinib Hydrochloride

目录号
EY2205
EY2205
EY2205
EY2205
EY2205
纯度
99.25%
99.25%
99.25%
99.25%
99.25%
规格
1 mg
5 mg
10 mg
25 mg
50 mg
原价
155
310
498
892
1360
售价
155
310
498
892
1360
库存
现货
现货
现货
现货
现货
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订购
订购
订购
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  • 生物活性

    Ponatinib HCL 是一种新型有效的多靶点抑制剂，在无细胞试验中作用于Abl，PDGFRα，VEGFR2，FGFR1和Src，IC50分别为0.37 nM，1.1 nM，1.5 nM，2.2 nM和5.4 nM。

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 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] Andrew P. Garner,et al. Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients. Clin Cancer Res. Author manuscript; available in PMC 2015 Nov 15. Published in final edited form as: Clin Cancer Res. 2014 Nov 15; 20(22): 5745–5755. Published online 2014 Sep 19. doi: 10.1158/1078-0432.CCR-14-1397.
    [2] Seiichi Okabe,et al. Combining the ABL1 Kinase Inhibitor Ponatinib and the Histone Deacetylase Inhibitor Vorinostat: A Potential Treatment for BCR-ABL-Positive Leukemia. PLoS One. 2014; 9(2): e89080. Published online 2014 Feb 28. doi: 10.1371/journal.pone.0089080.
    [3] Mingqiang Ren,et al. The novel BCR-ABL and FLT3 inhibitor ponatinib is a potent inhibitor of the multidrug resistance-associated ATP-binding cassette transporter ABCG2. Leukemia. Author manuscript; available in PMC 2013 Jul 1. Published in final edited form as: Leukemia. 2013 Jan; 27(1): 32–40. Published online 2012 Jul 11. doi: 10.1038/leu.2012.188.

    分子式
    C29H28ClF3N6O    		 分子量
    569.02    		 CAS号
    1114544-31-8    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    		 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
    NCT01746836 Leukemia Drug: Ponatinib M.D. Anderson Cancer Center|Ariad Pharmaceuticals Phase 2 2013-01-01 2016-11-16
    NCT01761747 Non-Small Cell Lung Cancer, Head and Neck Cancer Drug: ponatinib Dana-Farber Cancer Institute Phase 2|Phase 3 2013-01-01 2014-12-13
    NCT02428543 Acute Myeloid Lukemia Drug: Ponatinib and Cytarabine Versailles Hospital Phase 1|Phase 2 2013-07-01 2016-08-19
    NCT01888562 Endometrial Neoplasms Drug: Ponatinib Washington University School of Medicine 2016-01-01 2015-12-17
    NCT01935336 Adenocarcinoma of the Lung|Extensive Stage Small Cell Lung Cancer|Limited Stage Small Cell Lung Cancer|Recurrent Non-small Cell Lung Cancer|Recurrent Small Cell Lung Cancer|Stage IIIA Non-small Cell Lung Cancer|Stage IIIB Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer Drug: Ponatinib University of Colorado, Denver|Ariad Pharmaceuticals Phase 2 2013-09-01 2016-11-07
    NCT02265341 Malignant Hepatobiliary Neoplasm Other: Laboratory Biomarker Analysis|Drug: Ponatinib Hydrochloride|Other: Quality-of-Life Assessment Mayo Clinic|National Cancer Institute (NCI) Phase 2 2014-12-01 2016-12-20
    NCT02272998 Malignant Neoplasm Drug: ponatinib hydrochloride|Other: laboratory biomarker analysis Sameek Roychowdhury|Ohio State University Comprehensive Cancer Center Phase 2 2015-02-01 2016-05-06
    NCT01592136 Chronic Myeloid Leukemia (CML)|Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia (Ph+ ALL) Drug: ponatinib Ariad Pharmaceuticals 2013-03-12
    NCT01570868 Leukemia Drug: Ponatinib M.D. Anderson Cancer Center|Ariad Pharmaceuticals Phase 2 2012-04-01 2016-05-13
    NCT00660920 Chronic Myelogenous Leukemia|Hematologic Malignancies Drug: Ponatinib Ariad Pharmaceuticals Phase 1 2008-05-01 2016-02-12
    NCT01667133 Chronic Myeloid Leukemia (CML)|Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia (Ph+ ALL) Drug: ponatinib - Phase 1|Drug: ponatinib - Phase 2 Ariad Pharmaceuticals Phase 1|Phase 2 2012-08-01 2014-08-26
    NCT02627677 Chronic Phase Chronic Myeloid Leukemia Drug: ponatinib 30 mg QD|Drug: ponatinib 15 mg QD|Drug: nilotinib 400 mg BID Ariad Pharmaceuticals Phase 3 2015-12-01 2015-12-09
    NCT02478164 Glioblastoma Drug: Ponatinib Dana-Farber Cancer Institute Phase 2 2015-07-01 2016-10-11
    NCT02467270 Myeloid Leukemia, Chronic, Chronic Phase Drug: ponatinib 45 mg|Drug: ponatinib 30 mg|Drug: ponatinib 15 mg Ariad Pharmaceuticals Phase 2 2015-06-01 2017-03-02
    NCT01207440 Chronic Myeloid Leukemia|Ph+ Acute Lymphoblastic Leukemia Drug: Ponatinib Ariad Pharmaceuticals Phase 2 2010-09-01 2016-10-28
    NCT01549548 Philadelphia Chromosome Positive (Ph+) Leukemias|Chronic Myeloid Leukemia Drug: Ponatinib OHSU Knight Cancer Institute|Ariad Pharmaceuticals null 2013-03-13
    NCT02829840 Leukemia|FLT3-Mutated Acute Myeloid Leukemia|FLT3-Mutated High-Risk Myelodysplastic Syndrome Drug: Ponatinib|Drug: 5-azacytidine|Behavioral: Phone Calls M.D. Anderson Cancer Center|Ariad Pharmaceuticals Phase 1|Phase 2 2016-09-01 2016-08-05
    NCT01874665 GIST Drug: ponatinib Ariad Pharmaceuticals Phase 2 2013-06-01 2016-10-27
    NCT01813734 Non Small Cell Lung Cancer Drug: Ponatinib Massachusetts General Hospital Phase 2 2013-09-01 2016-09-12
    NCT02398825 Chronic Myeloid Leukemia|Chronic Phase|Adults Drug: Ponatinib Gruppo Italiano Malattie EMatologiche dell'Adulto Phase 2 2016-08-01 2016-09-14
    NCT01641107 Philadelphia Positive|BCR-ABL Positive|Acute Lymphoblastic Leukemia Drug: Ponatinib Gruppo Italiano Malattie EMatologiche dell'Adulto Phase 2 2014-10-01 2016-09-14
    NCT01838642 Thyroid Neoplasms Drug: Ponatinib National Institutes of Health Clinical Center (CC)|National Cancer Institute (NCI) Phase 2 2013-03-01 2016-12-30
    NCT02981784 Leukemia Drug: Ponatinib (Iclusig)|Procedure: allogeneic stem cell transplantation Hospices Civils de Lyon 2000-01-01 2016-12-01
    NCT01650805 Chronic Myeloid Leukemia Drug: ponatinib|Drug: imatinib (Gleevec/ Glivec) Ariad Pharmaceuticals Phase 3 2012-06-01 2014-11-05
    NCT02776605 ALL Drug: Prednisone|Drug: Vincristine|Drug: Daunorubicin|Drug: Prednisone|Drug: Ponatinib|Drug: Mercaptopurine|Drug: Methotrexate|Drug: VP-16|Drug: ARA-C:|Drug: TIT|Drug: Ponatinib|Procedure: Autologous transplantation|Procedure: Allo transplantation PETHEMA Foundation Phase 2 2016-06-01 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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