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Momelotinib Mesylate

CAS No. : 1056636-07-7

MCE 站：Momelotinib Mesylate

产品活性：Momelotinib Mesylate (CYT387 Mesylate) 是一种 ATP 竞争性的 JAK1/JAK2 抑制剂，IC₅₀ 值分别为 11 nM/18 nM，对其选择性约是 JAK3 的 10 倍。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling  |  Autophagy

作用靶点：JAK  |  Autophagy

In Vitro: Momelotinib Mesylate is an inhibitor of JAK1/JAK2 with IC₅₀ of 11 nM/18 nM, appr 10-fold selectivity versus JAK3. Momelotinib inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC₅₀ of 1400 nM. Furthermore, Momelotinib also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC₅₀ of 200 nM, 1 nM and 700 nM, respectively. In addition, Momelotinib has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC₅₀ of 2 μM-4 μM. Momelotinib inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, Momelotinib induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) cells.

In Vivo: In a murine MPN model, Momelotinib normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines.

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