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  • A-674563 hydrochloride
    • A-674563 HCl
    货号: abs818558
    CAS号: 552325-73-2(free base)
    分子式: C22H23ClN4O
    分子量: 394.9
    产品说明书
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    货号-规格 货期 价格 数量
    abs818558-2mg 1-2周 ¥2117.00
    - +
    abs818558-5mg 1-2周 ¥3704.00
    - +
    大包装询价
    产品描述
    描述

    A-674563 hydrochloride is a potent and selective Akt1 inhibitor with Ki of 11 nM. 

    纯度
    98%
    储存/保存方法
    Store at -20°C
    基本信息
    别名
    A-674563 HCl
    外观
    White to off-white powder
    可溶性/溶解性
    DMSO : ≥ 30 mg/mL (75.97 mM)
    生物活性
    靶点
    Akt1,CDK2,ERK2,GSK-3β,PKA
    In vitro(体外研究)
    A-674563 slows proliferation of tumor cells with an EC50 of 0.4 μM. A563 (0-10 µM) significantly decreases GSK3 and MDM2 phosphorylation in STS cells. A563 shows inhibitory effect on all STS cell lines, with IC50 values at 48 hours ranging from 0.22±0.034 µM (SW684) to 0.35 ±0.06 µM (SKLMS1). A563 induces G2 cell cycle arrest and apoptosis in STS cells. A563 (1 µM/12 hr) upregulates the expression of GADD45A independent of p53. A-674563 (10-1000 nM) is anti-proliferative and cytotoxic in cultured human melanoma cells, induces melanoma cell apoptotic death, inhibited by caspase inhibitors, and inhibits melanoma cells via Akt-dependent and -independent mechanisms. A-674563 is cytotoxic and anti-proliferative when added to U937 and AmL progenitor cells, activates caspase-3/9 and apoptosis in U937 and AmL progenitor cells, and manipulates other signalings in AmL cells whiling blocking Akt.
    In vivo(体内研究)
    A-674563 (40 mg/kg/d, p.o.) shows no significant monotherapy activity, but the efficacy of the combination therapy (A-674563+paclitaxel) is significantly improved in the PC-3 prostate cancer xenograft model. A-674563 (20, 100 mg/kg) increases plasma insulin in an oral glucose tolerance test. A563 (20 mg/kg/bid; p.o.) exhibits slow tumor growth and a significant difference in tumor volume without significant weight loss of mice. A563-treated tumors express increased levels of GADD45α and decreased levels of PCNA (a nuclear marker for proliferation). Additionally, TUNEL assay staining levels (marker for apoptosis) increase in the A563-treated specimens. A-674563 (25, 100 mg/kg, lavage daily) potently inhibits A375 xenograft growth in mice. A-674563 (15, 40 mg/kg) injection inhibits U937 xenograft in vivo growth, and improves mice survival.
    参考文献
    参考文献
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