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  • Momelotinib Mesylate
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    Momelotinib Mesylate

    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。

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    Momelotinib Mesylate的二维码
    • 库存: 现货
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    • 5mg
      ¥925.00
      740.00
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    • 10mg
      ¥1350.00
      1080.00
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    • 50mg
      ¥3725.00
      2980.00
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    • 100mg
      ¥5800.00
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    • 货号: ajce57534
    • CAS: 1056636-07-7
    • 别名: CYT387 Mesylate
    • 分子式: C24H26N6O5S
    • 分子量: 510.57
    • 纯度: >98%
    • 溶解度: Soluble in DMSO
    • 储存: Store at -20°C
    • 库存: 现货

    Background

    Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3. JAK1|11 nM (IC50)|JAK2|18 nM (IC50)|JAK3|155 nM (IC50)


    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[1]. 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[2].


    In a murine MPN model, Momelotinib normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines[3].


    [1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445. [2]. Monaghan KA, et al. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia, 2011, 25(12), 1891-1899. [3]. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240.

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