BMS-911543

"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

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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.