Home > JAK  & JAK & JAK & JAK & > Momelotinib

Momelotinib

CYT387,LM-1149,CYT11387,CYT-387

CYT387是一种ATP竞争性JAK1/JAK2抑制剂,IC50为11 nM/18 nM,比作用于JAK3选择性约高10倍左右。

目录号
EY1741
EY1741
EY1741
EY1741
纯度
99.37%
99.37%
99.37%
99.37%
规格
5 mg
10 mg
50 mg
100 mg
原价
525
860
2310
3820
售价
525
860
2310
3820
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    CYT387 is a small-molecule, ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 and 18 nM respectively.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% propylene glycol

  • 激酶实验

  • 细胞实验

    0 -10 μM

  • 动物实验

    ≤50 mg/kg 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 AKm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] Pardanani A, et al. Leukemia, 2009, 23(8), 1441-1445.

    分子式
    C23H22N6O2
    分子量
    414.46
    CAS号
    1056634-68-4
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    75 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
    NCT02124746 Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis|Polycythemia Vera|Essential Thrombocythemia Drug: Momelotinib Gilead Sciences Phase 2 2014-04-01 2017-02-28
    NCT01998828 Polycythemia Vera|Essential Thrombocythemia Drug: Momelotinib Gilead Sciences Phase 2 2014-02-01 2016-04-26
    NCT02101268 Primary Myelofibrosis (PMF)|Post-polycythemia Vera (Post-PV)|Post-essential Thrombocythemia Myelofibrosis (Post-ET MF) Drug: Momelotinib|Drug: Best Available Therapy (BAT) Gilead Sciences Phase 3 2014-06-01 2017-02-13
    NCT01969838 Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis Drug: Momelotinib|Drug: Ruxolitinib|Drug: Placebo to match momelotinib|Drug: Placebo to match ruxolitinib Gilead Sciences Phase 3 2013-12-01 2017-01-05
    NCT02101021 Metastatic Pancreatic Ductal Adenocarcinoma Drug: Momelotinib|Drug: Placebo to match momelotinib|Drug: Nab-paclitaxel|Drug: Gemcitabine Gilead Sciences Phase 3 2014-06-02 2017-03-21
    NCT01423058 Primary Myelofibrosis|Post-Polycythemia Vera|Post-Essential Thrombocythemia Myelofibrosis Drug: Momelotinib Gilead Sciences Phase 1|Phase 2 2011-08-01 2015-01-16
    NCT02515630 Primary Myelofibrosis (PMF)|Post-polycythemia Vera (Post-PV) Myelofibrosis|Postessential Thrombocythemia (Post-ET) Myelofibrosis Drug: MMB Gilead Sciences Phase 2 2016-01-29 2017-02-16
    NCT02244489 Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma Drug: MMB|Drug: Capecitabine|Drug: Oxaliplatin Gilead Sciences Phase 1 2014-11-01 2016-12-21
    NCT02258607 Relapsed Metastatic KRAS-Mutated Non-Small Cell Lung Cancer Drug: MMB|Drug: Trametinib Gilead Sciences Phase 1 2015-03-01 2016-08-04
    NCT02206763 EGFR Mutated EGFR TKI Naive Metastatic NSCLC Drug: MMB|Drug: Erlotinib Gilead Sciences Phase 1 2014-10-16 2017-03-20
    NCT01236638 Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis Drug: Momelotinib Gilead Sciences Phase 2 2010-11-01 2014-07-11
    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。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 :
  • 收件地址 :
  • 电话号码 :
  • 单位名称 :
  • 产品货号 :
  • 产品规格 :
  • 发票抬头以及单位税号 :