MyD88的二聚化抑制剂。
FAK Inhibitor 14 displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI. FAK Inhibitor 14 promotes cell detachment and inhibits cell adhesion in vitro, and exhibits antiproliferative activity in a variety of human tumor cell lines in vitro and in breast cancer cells in vivo.
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] Fanto, Nicola; Gallo, Grazia; Ciacci, Andrea et al. Design, Synthesis, and In Vitro Activity of Peptidomimetic Inhibitors of Myeloid Differentiation Factor 88. Journal of Medicinal Chemistry (2008), 51(5), 1189-1202.
[2] Loiarro, Maria; Capolunghi, Federica; Fanto, Nicola et al. Pivotal advance: inhibition of MyD88 dimerization and recruitment of IRAK1 and IRAK4 by a novel peptidomimetic compound. Journal of Leukocyte Biology (2007), 82(4), 801-810.
分子式 C27H28Cl2N4O5S |
分子量 591.51 |
CAS号 894787-30-5 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 10 mM |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00788528 | Obesity | Drug: S-2367 (velneperit) | Shionogi|Shionogi Inc. | Phase 2 | 2008-08-01 | 2011-09-13 |
NCT00153062 | Stroke | Drug: Aggrenox|Drug: Aggrenox|Drug: Clopidogrel placebo|Drug: Clopidogrel placebo|Drug: Micardis|Drug: Micardis|Drug: Aggrenox placebo|Drug: Aggrenox placebo|Drug: Clopidogrel|Drug: Clopidogrel|Drug: Micardis placebo|Drug: Micardis placebo | Boehringer Ingelheim|GlaxoSmithKline|Bayer | Phase 4 | 2003-08-01 | 2014-04-22 |
NCT00856284 | Type 2 Diabetes Mellitus | Drug: Alogliptin|Drug: Metformin|Drug: Glipizide | Takeda | Phase 3 | 2009-03-01 | 2013-09-25 |
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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