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  • NVP-BKM120(Buparlisib)

    促销商品
    • NVP-BKM-120, BKM-120; Buparlisib; BKM120; BKM 120
    货号: abs810586
    CAS号: 944396-07-0
    分子式: C18H21F3N6O2
    分子量: 410.39
    产品说明书
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    货号-规格 货期 价格 数量
    abs810586-5mg 现货 ¥873.00 ¥262.00
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    abs810586-50mg 现货 ¥3182.00 ¥955.00
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    大包装询价
    产品描述
    描述

    BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ.

    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
    NVP-BKM-120, BKM-120; Buparlisib; BKM120; BKM 120
    外观
    Powder
    可溶性/溶解性
    DMSO :76 mg/mL (185.2 mM)

    Ethanol :2 mg/mL (4.87 mM)
    生物活性
    靶点
    p110α ,p110δ ,p110β ,p110γ ,Vps34
    In vitro(体外研究)
    BKM120 is not sensitive to Class III and Class IV PI3K's or PI4K. NVP-BKM120 shows great antiproliferation activity to PI3K deregulated cell lines including A2780, U87MG, MCF7 and DU145 with GI50 of 0.1-0.7 nM. BKM120 induces multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266) apoptosis, which results in increased G1-phase cells and decreased S-phase cells. BKM120 induced CD138+ primary MM cell apoptosis and has significant lower cytotoxicity toward CD138− stromal cells. BKM120 exposure could cause upregulation of BimS and downregulation of XIAP. BKM120 demonstrates antiproliferative activity in human gastric cancer cell lines by decreasing mTOR downstream signaling. BKM120 could increase either p-ERK or p-STAT3 in KRAS mutant gastric cancer cells. Combination with STAT3 blockade, BKM120 shows a synergism in cells harboring mutated KRAS by inducing apoptosis, but not in KRAS wild-type cells. A recent study shows that BKM120 shows differential forms of cell death on the basis of p53 status of the cells with p53 wild-type cells undergoing apoptotic cell death and p53 mutant/deleted cells having a mitotic catastrophe cell death. BKM120 mediates mitotic catastrophe mainly through Aurora B kinase.
    In vivo(体内研究)
    BKM120 completely inhibits pAktser473 in A2780 xenograft tumors at doses of 30, 60, or 100 mg/kg, respectively. BKM120 also shows antitumor activity against U87MG glioma model at doses of 30 and 60 mg/kg. BKM120 treatment results in significantly reduced tumor volume and level of circulating human kappa chain at 5 μM/kg/day−1in ARP1 SCID mouse model, with prolonged survival.
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    • 实验方法 实验条件
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