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  • Ruxolitinib

    • 鲁索利替尼;Ruxolitinib;INCB 018424; INCB018424; INCB-018424
    货号: abs810523
    CAS号: 941678-49-5
    分子式: C17H18N6
    分子量: 306.37
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    货号-规格 货期 价格 数量
    abs810523-5mg 现货 ¥536.00
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    abs810523-10mg 现货 ¥737.00
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    abs810523-50mg 现货 ¥2867.00
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    abs810523-100mg 现货 ¥3226.00
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    大包装询价
    产品描述
    描述

    Ruxolitinib is a potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively and is relatively less selective for JAK3 (IC50 = 322 nM).

    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
    鲁索利替尼;Ruxolitinib;INCB 018424; INCB018424; INCB-018424
    外观
    White to Off-white powder
    可溶性/溶解性
    DMSO :61 mg/mL (199.1 mM)

    Ethanol :61 mg/mL (199.1 mM)
    生物活性
    靶点
    JAK2;JAK1
    In vitro(体外研究)
    INCB018424 potently and selectively inhibits JAK2V617F-mediated signaling and proliferation in Ba/F3 cells and HEL cells. INCB018424 markedly increases apoptosis in a dose dependent manner in Ba/F3 cells. INCB018424 (64 nM) results in a doubling of cells with depolarized mitochondria in Ba/F3 cells. INCB018424 inhibits proliferating of erythroid progenitors from normal donors and polycythemia vera patients with IC50 of 407 nM and 223 nM, respectively. INCB018424 demonstrates remarkable potency against erythroid colony formation with IC50 of 67nM.
    In vivo(体内研究)
    INCB018424 (180 mg/kg, orally, twice a day) results in survive rate of greater than 90% by day 22 in a JAK2V617F-driven mouse model. INCB018424 (180 mg/kg, orally, twice a day) markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminated neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects in a JAK2V617F-driven mouse model. The primary end point is reached in 41.9% of patients in the Ruxolitinib group as compared with 0.7% in the placebo group in the double-blind trial of myelofibrosis. Ruxolitinib results in maintaining of reduction in spleen volume and improvement of 50% or more in the total symptom score. A total of 28% of the patients in the Ruxolitinib (15 mg twice daily) group has at least a 35% reduction in spleen volume at week 48 in patients with myelofibrosis, as compared with 0% in the group receiving the best available therapy. The mean palpable spleen length has decreased by 56% with Ruxolitinib but has increased by 4% with the best available therapy at week 48. Patients in the ruxolitinib group has an improvement in overall quality-of-life measures and a reduction in symptoms associated with myelofibrosis.
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    • 实验方法 实验条件
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