"目录号: HY-15270
EpigeneticsStem Cell/WntJAK/STAT Signaling-
BMS-911543是JAK2抑制剂，对依赖于JAK2信号通路的细胞有抗增殖活性。
JAK
相关产品
Ruxolitinib-Baricitinib-Tofacitinib citrate-AZD-1480-WP1066-CYT387-Pacritinib-GLPG0634-Cerdulatinib-AT9283-Decernotinib-LY2784544-TG-101348-Upadacitinib-Itacitinib-
生物活性
Description
BMS-911543 is a potent and selective small-molecule inhibitor of JAK2, displays potent anti-proliferative and pharmacodynamic (PD) effects in cell lines dependent upon JAK2 signaling.IC50 value:Target: JAK2BMS-911543 displays potent anti-proliferative and pharmacodynamic (PD) effects in cell lines dependent upon JAK2 signaling, and has little activity in cell types dependent upon other pathways, such as JAK1 and JAK3. BMS-911543 also displays anti-proliferative responses in colony growth assays using primary progenitor cells isolated from patients with JAK2(V617F)-positive myeloproliferative neoplasms (MPNs). Similar to these in vitro observations, BMS-911543 is also highly active in in vivo models of JAK2 signaling, with sustained pathway suppression being observed after a single oral dose.
Clinical Trial
NCT01236352
Bristol-Myers Squibb
Cancer
April 2011
Phase 1-Phase 2
NCT01236352
Bristol-Myers Squibb
Cancer
April 2011
Phase 1-Phase 2
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References
[1].Purandare AV, et al. Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. Leukemia. 2012 Feb;26(2):280-8.
[2].Furqan M, et al. Dysregulation of JAK-STAT pathway in hematological malignancies and JAK inhibitors for clinical application. Biomark Res. 2013 Jan 16;1(1):5.