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产品描述： NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively |
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靶点：
JAK2 JH1:0.48 nM (IC50);FL JAK2 V617F:0.56 nM (IC50);FL JAK2 wt:0.58 nM (IC50);TYK2 JH1:10.76 nM (IC50);JAK3 JH1:18.68 nM (IC50);JAK1 JH1:31.63 nM (IC50);TyrosineKinases;JAK |
体内研究：
NVP-BSK805 (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell-driven mouse model. NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice |
参考文献：
1. Baffert F, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010 Jul;9(7):1945-55. 2. Cheon JH, et al. The JAK2 inhibitors CEP-33779 and NVP-BSK805 have high P-gp inhibitory activity and sensitize drug-resistant cancer cells to vincristine. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1176-1182. |
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溶解性：
Soluble in DMSO |
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保存条件：
-20℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
2.039 ml |
10.193 ml |
20.385 ml |
| 5 mM |
0.408 ml |
2.039 ml |
4.077 ml |
| 10 mM |
0.204 ml |
1.019 ml |
2.039 ml |
| 50 mM |
0.041 ml |
0.204 ml |
0.408 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京