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  • BIIB-021

    • CNF2024
    货号: abs817470
    CAS号: 848695-25-0
    分子式: C14H15ClN6O
    分子量: 318.762
    产品说明书
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    货号-规格 货期 价格 数量
    abs817470-5mg 1-2周 ¥758.00
    - +
    abs817470-10mg 1-2周 ¥1335.00
    - +
    abs817470-50mg 1-2周 ¥3439.00
    - +
    abs817470-100mg 1-2周 ¥6015.00
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    大包装询价
    产品描述
    描述

    BIIB021 是一种合成的 HSP90 抑制剂,Ki 值和 EC50 值分别为 1.7 nM 和 38 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
    CNF2024
    可溶性/溶解性
    DMSO ≥60mg/mL
    生物活性
    靶点
    HSP90
    In vitro(体外研究)
    BIIB021 binds in the ATP-binding pocket of Hsp90, interferes with Hsp90 chaperone function, and results in client protein degradation and tumor growth inhibition. BIIB021 inhibits tumor cell (BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82) proliferation with IC50 from 0.06-0.31 μM. BIIB021 induces the degradation of Hsp90 client proteins including HER-2, Akt, and Raf-1 and up-regulated expression of the heat shock proteins Hsp70 and Hsp27. BIIB021 inhibits Hodgkin's lymphoma cells (KM-H2, L428, L540, L540cy, L591, L1236 and DEV) with IC50 from 0.24-0.8 μM. BIIB021 shows low activity in lymphocytes from healthy individuals. BIIB021 inhibits the constitutive activity of NF-κB despite defective IκB. BIIB021 induces the expression of ligands for the activating NK cell receptor NKG2D on Hodgkin's lymphoma cells resulting in an increased susceptibility to NK cell–mediated killing. BIIB021 enhanced the in vitro radiosensitivity of HNSCCA cell lines (UM11B and JHU12) with a corresponding reduction in the expression of key radioresponsive proteins, increased apoptotic cells and enhance G2 arrest. BIIB021 is considerably more active than 17-AAG against adrenocortical carcinoma H295R, both in vitro and in vivo. The cytotoxic activity of BIIB021 is not influenced by loss of NQO1 or Bcl-2 overexpression, molecular lesions that do not prevent client loss but are nonetheless associated with reduced cell killing by 17-AAG. BIIB021 is also active in 17-AAG resistant cell lines (NIH-H69, MES SA Dx5, NCI-ADR-RES, Nalm6 and etc.).
    In vivo(体内研究)
    Oral administration of BIIB021 leads to tumor growth inhibition in many tumor xenograft models including N87, BT474, CWR22, U87, SKOV3 and Panc-1. BIIB021 effectively inhibits growth of L540cy tumor at a dose of 120 mg/kg. BIIB021 significantly enhances antitumor growth effect of radiation in JHU12 xenograft.
    参考文献
    参考文献
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    • 实验方法 实验条件
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