S84209 |
NSC 42834 |
源叶(MedMol) | 98% |
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- 产品描述: NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
- 靶点: JAK2-WT:15 μM (IC50);JAK2-V617F:28 μM (IC50)
- 体外研究:
NSC 42834 (JAK2 Inhibitor V) selectively inhibited Jak2 kinase function with no effect on Tyk2 or c-Src kinase function. NSC 42834 significantly inhibited proliferation of the Jak2-V617F-expressing, human erythroleukemia cell line, HEL 92.1.7. The NSC 42834-mediated reduction in cell proliferation correlated with reduced Jak2 and STAT3 tyrosine phosphorylation levels as well as marked cell cycle arrest. Finally, NSC 42834 inhibited the growth of hematopoietic progenitor cells isolated from the bone marrow of an essential thrombocythemia patient harboring the Jak2-V617F mutation and a polycythemia vera patient carrying a Jak2-F537I mutation.
- 参考文献:
1. Jacqueline Sayyah, Andrew Magis, David A. Ostrov, et al. Z3, a novel Jak2 tyrosine kinase small-molecule inhibitor that suppresses Jak2-mediated pathologic cell growth . Mol Cancer Ther 2008;7(8):2308-18. 2. Jacqueline Sayyah, Peter P. Sayeski. Jak2 inhibitors: Rationale and role as therapeutic agents in hematologic malignancies. Current Oncology Reports. 2009, 11(2): 117-124. 3. Ehab Atallah , Srdan Verstovsek . Prospect of JAK2 inhibitor therapy in myeloproliferative neoplasms. Expert Review of Anticancer Therapy. 2009,9 (5):663-670.
- 溶解性: Soluble in DMSO、Ethanol
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.903 ml 14.516 ml 29.032 ml 5 mM 0.581 ml 2.903 ml 5.806 ml 10 mM 0.29 ml 1.452 ml 2.903 ml 50 mM 0.058 ml 0.29 ml 0.581 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)