离岸价格
获取最新报价( Negotiable )
|Minimum Order
位置:
china
最小订单价格:
-
最小订单:
100 Gram
包装细节:
Aluminum foil bag, PTFE Bottle, or meet your requirment
交货时间:
Within one week
供应能力:
100 Kilogram per Month
付款方式:
D/P, L/C, T/T
联系人 Mr. James
Building A, NO.688,Qiushi Road,Jinshan District, Shanghai, shanghai
| In vitro, masitinib had greater activity and selectivity against KIT than imatinib, inhibiting recombinant human wild-type KIT with an half inhibitory concentration (IC(*0)) of **0+/**0 nM and blocking stem cell factor-induced proliferation and KIT tyrosine phosphorylation with an IC(*0) of **0+/**0 nM in Ba/F3 cells expressing human or mouse wild-type KIT. Masitinib also potently inhibited recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. In contrast, masitinib demonstrated weak inhibition of ABL and c-Fms and was inactive against a variety of other tyrosine and serine/threonine kinases. This highly selective nature of masitinib suggests that it will exhibit a better safety profile than other tyrosine kinase inhibitors; indeed, masitinib-induced cardiotoxicity or genotoxicity has not been observed in animal studies. Molecular modelling and kinetic analysis suggest a different mode of binding than imatinib, and masitinib more strongly inhibited degranulation, cytokine production, and bone marrow mast cell migration than imatinib. Furthermore, masitinib potently inhibited human and murine KIT with activating mutations in the juxtamembrane domain. In vivo, masitinib blocked tumour growth in mice with subcutaneous grafts of Ba/F3 cells expressing a juxtamembrane KIT mutant. |
