NVP-BSK805 (hydrochloride)
货号：
16714-1mg 基本售价：
770.0 元 规格：
1 mg
产品信息
概述| 货号 | 16714-1mg |
| 描述 | Janus kinases (JAKs) are non-receptor tyrosine kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.1 A point mutation of JAK2, V617F, activates signaling through STAT5 and drives certain forms of cancer.2 NVP-BSK805 is a potent inhibitor of JAK2 that also inhibits the JAK2V617F mutant enzyme (IC50s for both enzymes ~ 0.5 nM). It displays at least 20-fold selectivity against other JAK enzymes and a panel of serine/threonine and tyrosine kinases.2 This ATP-competitive inhibitor is orally bioavailable and has a long half-life in vivo, suppressing leukemic cell spreading and splenomegaly in JAK2V617F cell-driven disease in mice.2 NVP-BSK805 suppresses recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.2 NVP-BSK805 can be used to study the molecular mechanisms involved in JAK2V617F signaling in cells.3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Yamaoka, K.,Saharinen, P.,Pesu, M., et al. The janus kinases (Jaks). Genome Biology 5(12), 1-6 (2004).
2.Baffert, F.,Régnier, C.H.,De Pover, A., et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Molecular Cancer Therapeutics 9(7), 1945-1955 (2010).
3.Rubert, J.,Qian, Z.,Andraos, R., et al. Bim and Mcl-1 exert key roles in regulating JAK2V617F cell survival. BMC Cancer 11, 2-14 (2011).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 563.5 |
| 分子式 | C27H28F2N6O • 2HCl |
| 稳定性 | ≥ 2 years |
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