Masitinib, a novel phenylaminothiazole-type derivative, is an inhibitor of the class III receptor tyrosine kinase stem-cell growth factor receptor (c-Kit) with IC50 of 200 nM, platelet-derived growth factor receptor α and β and the non-receptor tyrosine kinase Lyn(PDGFRα/β with IC50 of 540 nM/800 nM).
In a Phase II trial, masitinib has been reported to significantly increase the overall survival rate and progression-free survival in patients with locally advanced or metastatic gastrointestinal stromal tumor.
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] Milan Milovancev,et al. Antiproliferative effects of masitinib and imatinib against canine oral fibrosarcoma in vitro. BMC Vet Res. 2016; 12: 85. Published online 2016 Jun 4. doi: 10.1186/s12917-016-0712-x.
[2] Ivan Kocic,et al. Neuroprotective effect of masitinib in rats with postischemic stroke. Naunyn Schmiedebergs Arch Pharmacol. 2015; 388: 79–86. Published online 2014 Oct 26. doi: 10.1007/s00210-014-1061-6.
分子式 C28H30N6OS |
分子量 498.64 |
CAS号 790299-79-5 |
储存方式 -20 ℃长期冷藏储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mg/mL |
Water <1 mg/mL |
Ethanol 4 mg/mL |
体内溶解度
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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