2. PI3K/Akt/mTOR
  3. Akt
  4. A-674563 hydrochloride

A-674563 hydrochloride 

目录号: HY-13254A 纯度: 99.86%
COA 产品使用指南

摩尔计算器

A-674563 hydrochloride 是具有选择性的高效 Akt1 抑制剂，其 Ki 值为 11 nM。

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A-674563 hydrochloride Chemical Structure

A-674563 hydrochloride Chemical Structure

CAS No. : 2070009-66-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1540
In-stock
1 mg ￥600
In-stock
5 mg ￥1400
In-stock
10 mg ￥2200
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of A-674563 hydrochloride:

A-674563 hydrochloride 相关抗体

Top Publications Citing Use of Products

    A-674563 hydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2016 May 17;7(20):29131-42.  [Abstract]

    A674563 selectively inhibits FLT3-ITD. Inhibitory Effects of A674563 against auto-phosphorylation of FLT3 wt/mt kinases in the FLT3 wt/mt transformed BaF3 isogenic cell lines.

    查看 Akt 亚型特异性产品:

    查看所有亚型
    Akt Akt1 Akt2 Akt3

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

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

    IC50 & Target[1]

    Akt1

    11 nM (Ki)

    PKA

    16 nM (Ki)

    CDK2

    46 nM (Ki)

    GSK3β

    110 nM (Ki)

    ERK2

    260 nM (Ki)

    PKCδ

    360 nM (Ki)

    RSK2

    580 nM (Ki)

    MAPK-AP2

    1.1 μM (Ki)

    PKCγ

    1.2 μM (Ki)

    Chk1

    2.6 μM (Ki)

    CK2

    5.4 μM (Ki)

    SRC

    13 μM (Ki)

    体外研究
    (In Vitro)

    A-674563 slows proliferation of tumor cells with an EC50 of 0.4 μM[1]. 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[2]. 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[3]. 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[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    A-674563 hydrochloride 相关抗体:
    体内研究
    (In Vivo)

    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[1]. 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[2]. A-674563 (25, 100 mg/kg, lavage daily) potently inhibits A375 xenograft growth in mice[3]. A-674563 (15, 40 mg/kg) injection inhibits U937 xenograft in vivo growth, and improves mice survival[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    394.90

    Formula

    C22H23ClN4O
    CAS 号
    性状

    固体

    颜色

    Light yellow to khaki

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    溶解性数据
    In Vitro: 

    H2O 中的溶解度 : 100 mg/mL (253.23 mM; 超声助溶)

    DMSO 中的溶解度 : 50 mg/mL (126.61 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5323 mL 12.6614 mL 25.3229 mL
    5 mM 0.5065 mL 2.5323 mL 5.0646 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.27 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (5.27 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    以下溶解方案，请直接配置工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： PBS

      Solubility: 100 mg/mL (253.23 mM); 澄清溶液; 超声助溶 (<60°C)

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.86%

    COA (263 KB) HNMR (290 KB) LCMS (96 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    The cells on 96-well plates are gently washed with 200 μL of PBS. Alamar Blue reagent is diluted 1:10 in normal growth media. The diluted Alamar Blue reagent (100 μL) is added to each well on the 96-well plates and incubated until the reaction is complete. Analysis is done using an fmax Fluorescence Microplate Reader, set at the excitation wavelength of 544 nm and emission wavelength of 595 nm. Data are analyzed using SOFTmax PRO software.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Immunocompromised male scid mice are at 6 to 8 weeks of age. The 1×106 3T3-Akt1 or 2×106 MiaPaCa-2 and PC-3 cells in 50% Matrigel are inoculated s.c. into the flank. For early treatment studies, mice are randomLy assigned to treatment groups and therapy is initiated the day after inoculation. Ten animals are assigned to each group, including controls. For established tumor studies, tumors are allowed to reach a designated size and mice are assigned to treatment groups of equal tumor size (n=10 mice per group). Tumor size is evaluated by twice weekly measurements with digital calipers. Tumor volume is estimated using the formula: V=L×W2/2. A-443654 is given s.c. in a vehicle of 0.2% HPMC. A-674563 is given orally in a vehicle of 5% dextrose. Gemcitabine and paclitaxel are added to the assay.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    A-674563 hydrochloride 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 2.5323 mL 12.6614 mL 25.3229 mL 63.3072 mL
    5 mM 0.5065 mL 2.5323 mL 5.0646 mL 12.6614 mL
    10 mM 0.2532 mL 1.2661 mL 2.5323 mL 6.3307 mL
    15 mM 0.1688 mL 0.8441 mL 1.6882 mL 4.2205 mL
    20 mM 0.1266 mL 0.6331 mL 1.2661 mL 3.1654 mL
    25 mM 0.1013 mL 0.5065 mL 1.0129 mL 2.5323 mL
    30 mM 0.0844 mL 0.4220 mL 0.8441 mL 2.1102 mL
    40 mM 0.0633 mL 0.3165 mL 0.6331 mL 1.5827 mL
    50 mM 0.0506 mL 0.2532 mL 0.5065 mL 1.2661 mL
    60 mM 0.0422 mL 0.2110 mL 0.4220 mL 1.0551 mL
    80 mM 0.0317 mL 0.1583 mL 0.3165 mL 0.7913 mL
    100 mM 0.0253 mL 0.1266 mL 0.2532 mL 0.6331 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    A-6745632070009-66-2A674563A 674563AktPKBProtein kinase BInhibitorinhibitorinhibit

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