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  • Momelotinib (CYT387,CYT-387)

    • CYT 11387,CYT387 (CYT 387),momelotinib
    货号: abs810565
    CAS号: 1056634-68-4
    分子式: C23H22N6O2
    分子量: 414.46
    产品说明书
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    货号-规格 货期 价格 数量
    abs810565-5mg 现货 ¥979.00
    - +
    abs810565-10mg 现货 ¥1272.00
    - +
    abs810565-50mg 现货 ¥3514.00
    - +
    abs810565-100mg 现货 ¥5931.00
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    大包装询价
    产品描述
    描述

    CYT387 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50 of 11 nM and 18 nM, respectively.

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    CYT 11387,CYT387 (CYT 387),momelotinib
    外观
    Powder
    可溶性/溶解性
    DMSO 74 mg/mL (178.54 mM)






    生物活性
    靶点
    JAK1 ,JAK2 ,JAK3
    In vitro(体外研究)
    CYT387 inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, CYT387 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, CYT387 has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2μ-4 μM. A recent study shows that CYT387 inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, CYT387 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(体内研究)
    In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines.
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    • 实验方法 实验条件
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