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- 英文名：
CYT387 Mesylate
- 库存：
货期：电询
- 供应商：
MedChemExpress LLC
- CAS号：
1056636-07-7
- 规格：
电询
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Momelotinib Mesylate
CAS No. : 1056636-07-7
MCE 国际站：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 | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt | 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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