TG101348
货号：
16289-1mg 基本售价：
630.0 元 规格：
1 mg
产品信息
概述| 货号 | 16289-1mg |
| 描述 | Janus kinases (JAKs) are non-receptor kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.1JAK2V617F and MPLW515L/K are two known mutations that cause dysregulated JAK/STAT signaling in myeloproliferative disorders. TG101348 is a small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM).2 It can inhibit the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 value of 200 nM.2 Phase I clinical trial results that focused on safety and efficacy of TG101348 in patients with high- or intermediate-risk primary or post-polycythemia vera/essential thrombocythemia myelofibrosis have been published.3 |
| 别名 | Fedratinib;SAR302503; |
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.Pardanani, A.,Lasho, T.,Levine, R.L., et al. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia 21(8), 1658-1668 (2007).
3.Pardanani, A.,Gotlib, J.R.,Jamieson, C., et al. Safety and efficacy of TG101348, a selective JAK2 inhibitor, in myelofibrosis. Journal of Clinical Oncology 29(7), 789-796 (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 | 524.7 |
| 分子式 | C27H36N6O3S |
| CAS号 | 936091-26-8 |
| 稳定性 | ≥ 2 years |
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