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Pacritinib

SB1518,SB 1518,SB-1518

Pacritinib (SB1518)对JAK2WT，JAK2V617F，FLT3，JAK1和JAK3的IC50分别为23nM，19nM，22nM，1280nM和520nM。

目录号
EY0538
EY0538
EY0538
EY0538
纯度
99.64%
99.64%
99.64%
99.64%
规格
2 mg
5 mg
10 mg
25 mg
原价
608.00
768.00
1350.00
2400.00
售价
608.00
768.00
1350.00
2400.00
库存
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

    Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    150 mg/kg 口服灌胃

  • 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] Hart S, et al. Leukemia, 2011, 25(11), 1751-1759.
    [2] William AD, et al. Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma. J Med Chem. 2011 Jul 14;54(13):4638-58.
    [3] Novotny-Diermayr V, et al. The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib(SB1518) in preclinical models of AML. Blood Cancer J. 2012 May;2(5):e69.

    分子式
    C28H32N4O3    		 分子量
    472.58    		 CAS号
    937272-79-2     		储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    12 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

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

    NCT02532010 Acute Myeloid Leukemia (AML) Drug: Pacritinib|Drug: Decitabine|Drug: Cytarabine Weill Medical College of Cornell University Phase 2 2015-06-01 2016-02-17
    NCT02803762 Healthy Drug: Pacritinib CTI BioPharma|QPS-Qualitix Phase 1 2014-07-01 2016-06-14
    NCT02765724 Myelofibrosis Drug: Pacritinib CTI BioPharma|SGS S.A. Phase 1 2015-01-01 2016-05-04
    NCT02807116 Healthy Subjects Drug: Pacritinib|Drug: Rifampin|Drug: Pacritinib and Rifampin CTI BioPharma|Covance Phase 1 2015-01-01 2016-06-20
    NCT02807051 Drug Interaction Study Drug: Pacritinib|Drug: Clarithromycin|Drug: Pacritinib and Clarithromycin CTI BioPharma|Covance Phase 1 2014-09-01 2016-06-20
    NCT02277093 Colorectal Cancer Drug: Pacritinib Washington University School of Medicine|CTI BioPharma Phase 2 2015-09-01 2016-11-09
    NCT02677948 Chronic Lymphocytic Leukemia|Lymphoma, Small Lymphocytic Drug: Pacritinib|Drug: Ibrutinib University of Michigan Cancer Center Phase 1|Phase 2 2016-10-01 2016-09-01
    NCT02564536 Chronic Myelomonocytic Leukemia|Juvenile Myelomonocytic Leukemia|Atypical Chronic Myeloid Leukemia|Myeloproliferative Neoplasm|Myelodysplastic Syndromes|Myelofibrosis Drug: Pacritinib|Drug: Decitabine Washington University School of Medicine|CTI BioPharma Phase 1 2017-06-01 2017-03-03
    NCT02469415 Leukemia Drug: Pacritinib|Drug: 5-azacitidine|Drug: Decitabine M.D. Anderson Cancer Center|CTI BioPharma Phase 2 2015-09-01 2017-01-18
    NCT02323607 Recurrent Adult Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Therapy-Related Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia Drug: Pacritinib|Drug: Cytarabine|Drug: Daunorubicin Hydrochloride|Drug: Decitabine|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study Bhavana Bhatnagar|CTI BioPharma|Ohio State University Comprehensive Cancer Center Phase 1 2016-01-01 2016-07-14
    NCT02342353 Non-Small Cell Lung Cancer|Nonsmall Cell Lung Cancer|Carcinoma, Non-Small-Cell Lung Drug: Pacritinib|Drug: Erlotinib Washington University School of Medicine Phase 1|Phase 2 2015-05-18 2017-02-14
    NCT02891603 Graft Vs Host Disease|GVHD Drug: Pacritinib|Drug: Sirolimus|Drug: Tacrolimus H. Lee Moffitt Cancer Center and Research Institute Phase 1|Phase 2 2017-04-30 2017-01-25
    NCT02584777 Primary Myelofibrosis Biological: Pacritinib Baxalta US Inc.|CTI BioPharma Phase 2 2015-11-01 2016-07-08
    NCT01773187 Primary Myelofibrosis|Post-polycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis Drug: Pacritinib|Drug: Best Available Therapy CTI BioPharma Phase 3 2012-12-01 2016-12-15
    NCT02808455 Healthy Subjects Drug: Pacritinib 400 mg Capsule (Treatment A)|Drug: Pacritinib 80 mg Solution (Treatment B) CTI BioPharma|Covance Phase 1 2015-01-01 2016-06-16
    NCT02055781 Primary Myelofibrosis|Post-polycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis Drug: Pacritinib|Drug: Best Available Therapy CTI BioPharma Phase 3 2013-12-01 2016-12-15
    NCT02807077 Myelofibrosis Drug: Pacritinib CTI BioPharma|SGS S.A. Phase 1 2014-11-01 2016-06-20
    NCT02410551 Myeloproliferative Diseases Drug: Pacritinib|Drug: Busulfan|Behavioral: Questionnaires|Behavioral: Phone Calls|Procedure: Allogeneic Stem Cell Transplantation|Drug: Fludarabine M.D. Anderson Cancer Center|CTI BioPharma Phase 2 2015-06-15 2017-01-23
    NCT02823171 Healthy Drug: Treatment A: 400 mg Pacritinib P3CT|Drug: Treatment B: 400 mg of pacritinib FMI CTI BioPharma|Covance Phase 1 2015-08-01 2016-06-30
    NCT02807207 Healthy Subjects Drug: A: 400 mg pacritinib|Other: B: Placebo|Drug: C: 400 mg moxifloxacin CTI BioPharma|Covance Phase 1 2014-10-01 2016-06-16
    NCT02251821 Primary Myelofibrosis|Secondary Myelofibrosis Procedure: Allogeneic Hematopoietic Stem Cell Transplantation|Drug: Busulfan|Drug: Cyclophosphamide|Drug: Fludarabine Phosphate|Other: Laboratory Biomarker Analysis|Drug: Melphalan|Drug: Methotrexate|Drug: Momelotinib|Drug: Mycophenolate Mofetil|Drug: Pacritinib|Drug: Ruxolitinib|Drug: Tacrolimus|Radiation: Total-Body Irradiation|Procedure: Umbilical Cord Blood Transplantation Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI)|National Heart, Lung, and Blood Institute (NHLBI) Phase 2 2014-10-01 2016-11-29

    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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