R406是Syk抑制剂,IC50为41 nM,比对Flt3的抑制性强5倍。
SYK inhibitor,potent and ATP-competitive.
30% PEG400+0.5% Tween80+5% propylene glycol
1 或5 mg/kg 口服处理
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。
[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
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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