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R406

R406是Syk抑制剂,IC50为41 nM,比对Flt3的抑制性强5倍。

目录号
EY1351
EY1351
EY1351
EY1351
纯度
98.68%
98.68%
98.68%
98.68%
规格
2 mg
5 mg
10 mg
50 mg
原价
770
1100
1800
6180
售价
770
1100
1800
6180
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

    SYK inhibitor,potent and ATP-competitive.

  • 体外研究

  • 体内研究

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

  • 激酶实验

  • 细胞实验

  • 动物实验

    1 或5 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] Braselmann S, et al. J Pharmacol Exp Ther, 2006, 319(3), 998-1008.

    分子式
    C28H29FN6O8S
    分子量
    628.63
    CAS号
    841290-81-1
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    126 mg/mL
    Water
    <1 mg/mL
    Ethanol
    5 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
    NCT01645085 Healthy Volunteers Drug: MCC-based 13% drug loaded tablets|Drug: Mannitol-based 38% drug-loaded tablet|Drug: MCC-based 13% drug loaded tablets|Drug: Mannitol-based 38% drug-loaded tablet AstraZeneca Phase 1 2012-07-01 2013-03-18
    NCT01682408 Pharmacokinetics Drug: Fostamatinib - 1 x 150mg mannitol-based 38% drug-loaded tablet(orange reference)|Drug: Fostamatinib - 3 x 50mg microcrystalline cellulose-based 13% drug loaded tablets,(blue) fed|Drug: Fostamatinib - 1 x 150mg mannitol based 38% drug-loaded tablet (batch variant A)|Drug: Fostamatinib - 1 x 150mg mannitol based 38% drug loaded tablet (batch variant B)|Drug: Ranitidine AstraZeneca Phase 1 2012-09-01 2012-12-27
    NCT01598571 Healthy Drug: Fostamatinib|Drug: Fostamatinib AstraZeneca Phase 1 2012-05-01 2012-08-21
    NCT01222455 Hepatic Impairment|Healthy Volunteers|Pharmacokinetics|Amount of R406 in Blood Drug: Fostamatinib AstraZeneca Phase 1 2010-10-01 2011-07-05
    NCT01336218 Rheumatoid Arthritis|Healthy Volunteers Drug: fostamatinib|Drug: rifampicin AstraZeneca Phase 1 2011-04-01 2011-07-21
    NCT01197781 Drug Drug Interactions|Healthy Volunteers Drug: FOSTAMATIN|Drug: Verapamil AstraZeneca Phase 1 2010-09-01 2010-11-19
    NCT01245790 Rheumatoid Arthritis|Renal Impairment Drug: fostamatinib AstraZeneca Phase 1 2010-11-01 2011-06-15
    NCT01387308 Healthy Drug: Fostamatinib|Drug: Fostamatinib|Drug: Fostamatinib|Drug: Fostamatinib|Drug: Fostamatinib AstraZeneca Phase 1 2011-08-01 2011-10-27
    NCT01355354 Healthy Volunteers|Rheumatoid Arthritis Drug: Digoxin|Drug: Fostamatinib AstraZeneca Phase 1 2011-06-01 2011-10-05
    NCT01311622 Rheumatoid Arthritis|Healthy Subjects Drug: warfarin|Drug: fostamatinib AstraZeneca Phase 1 2011-03-01 2013-01-30
    NCT01208155 Bioavailability|Pharmacokinetics Drug: Fostamatinib|Drug: Fostamatinib|Drug: Fostamatinib|Drug: Fostamatinib AstraZeneca Phase 1 2010-09-01 2010-12-07
    NCT01725230 Rheumatoid Arthritis Drug: Fostamatinib|Drug: Rosuvastatin|Drug: Simvastatin AstraZeneca Phase 1 2012-11-01 2013-02-01

    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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