2. PI3K/Akt/mTOR
  3. Akt
  4. A-443654

A-443654 是一种有效的 pan-Akt 抑制剂，以同等效力抑制 Akt1，Akt2，和 Akt3，Ki 值均为 160 pM。

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A-443654 Chemical Structure

A-443654 Chemical Structure

CAS No. : 552325-16-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1749
In-stock
1 mg ￥829
In-stock
5 mg ￥2000
In-stock
10 mg ￥3120
In-stock
25 mg ￥5760
In-stock
50 mg 现货 询价
100 mg 现货 询价
200 mg 现货 询价
500 mg   询价  
1 g   询价  

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Customer Review

A-443654 相关抗体

Top Publications Citing Use of Products

    A-443654 purchased from MCE. Usage Cited in: CNS Neurosci Ther. 2018 Jun;24(6):495-507.  [Abstract]

    The MPP/PHTPP-and G15-induced decreases in p-AKT, AKT, and rictor expression are differently affected by mTORC2 activation with A-443654 in the adult female hippocampus.

    A-443654 purchased from MCE. Usage Cited in: CNS Neurosci Ther. 2018 Jun;24(6):495-507.  [Abstract]

    Immunohistochemistry results show that the MPP/PHTPP- and G15-induced dramatic decrease in profilin-1 expression is significantly reversed by A-443654.

    A-443654 purchased from MCE. Usage Cited in: J Steroid Biochem Mol Biol. 2017 Nov;174:96-113.  [Abstract]

    A443654 rescues the methylphenolpyrazole (MPP) + PHTPP-induced downregulation of p-AKT.

    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-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM)[1].

    IC50 & Target

    Akt1

    160 pM (Ki)

    Akt2

    160 pM (Ki)

    Akt3

    160 pM (Ki)

    PKA

    6.3 nM (Ki)

    PKCγ

    24 nM (Ki)

    PKCδ

    33 nM (Ki)

    KDR

    3.1 μM (Ki)

    cKIT

    1.2 μM (Ki)

    SRC

    2.6 μM (Ki)

    Flt1

    3.6 μM (Ki)

    CDK2

    24 nM (Ki)

    ERK2

    340 nM (Ki)

    GSK3β

    41 nM (Ki)

    CK2

    2.4 μM (Ki)

    Chk1

    2.3 μM (Ki)

    RSK2

    11 nM (Ki)

    MAPK-AP2

    3.3 μM (Ki)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK-293T IC50
    2.5 nM
    Compound: A-443654
    Inhibition of myristoylated wild type AKT1 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay
    Inhibition of myristoylated wild type AKT1 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay
    		[PMID: 19465931]
    HEK-293T IC50
    30 nM
    Compound: A-443654
    Inhibition of myristoylated wild type AKT2 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay
    Inhibition of myristoylated wild type AKT2 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay
    		[PMID: 19465931]
    HEK-293T IC50
    51 nM
    Compound: A-443654
    Inhibition of myristoylated wild type AKT3 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay
    Inhibition of myristoylated wild type AKT3 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay
    		[PMID: 19465931]
    体外研究
    (In Vitro)

    A-443654 exhibits a Ki of 160 pM, a 30,000-fold improvement in potency versus the initial lead molecule. A-443654 is 40-fold selective for Akt over PKA. A-443654 inhibits Akt1, Akt2, or Akt3 equally within cells. A-443654 reduces the P-GSK3 in a dose-responsive manner in all three cell lines. A-443654 inhibits the proliferation of tumor cells with EC50 of 0.1 μM[1]. A-443654-induced morphological changes occur very rapidly (within 2 to 4 h) in both 10A and 10CA1a cells, with 10CA1a cells more sensitive to A-443654 than the 10A cells. A-443654 alone at 2 μM causes the 10CA1a cells, but not the 10A cells, to detach from the plate after 12 h, whereas 1 μM of A-443654 causes 10CA1a cells to detach from the plate after 12 h. FACScan Analysis of rapamycin and A-443654 effects on DNA content in 10A and 10CA1a cells. In contrast, A-443654 at 2 and 5 μM decreases Bcl-2 levels by 30 to 40% in the 10CA1a cells at 8h. The combination of rapamycin with 2 or 5 μM A-443654, however, markedly decreases Bcl-2 protein levels by appr 40 to 50% in the 10A cells and by appr 70% in the 10CA1a cells, respectively[2]. A-443654 demonstrates the greatest selective effect on the mutant cells compared to the WT cells with greater than 3.5 fold relative growth inhibition of the mutant cells[3].

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

    A-443654 相关抗体:
    体内研究
    (In Vivo)

    A-443654 (7.5 mg/kg/d, s.c.) inhibits tumor growth in the 3T3-Akt1 flank tumor model. A-443654 (50 mg/kg, s.c.) induces apoptosis in 3T3-Akt1 flank tumors. A-443654 (30 mg/kg, s.c.) leads to increased levels of phosphorylated Akt1 in MiaPaCa-2 tumors[1].

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

    397.47

    Formula

    C24H23N5O
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (251.59 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5159 mL 12.5796 mL 25.1591 mL
    5 mM 0.5032 mL 2.5159 mL 5.0318 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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

    动物实验：

    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: ≥ 2.5 mg/mL (6.29 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.29 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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。

      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。
    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
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料
    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 as per manufacturer's instructions. Analysis is done using an fmaxFluorescence Microplate Reader, set at the excitation wavelength of 544 nm and emission wavelength of 595 nm. Data are analyzed using SOFTmax PRO software provided by the manufacturer.

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

    Immunocompromised male scid mice are 6 to 8 weeks of age. The 3T3-Akt1 cell line is developed and characterized in our laboratory. 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.

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

    A-443654 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5159 mL 12.5796 mL 25.1591 mL 62.8978 mL
    5 mM 0.5032 mL 2.5159 mL 5.0318 mL 12.5796 mL
    10 mM 0.2516 mL 1.2580 mL 2.5159 mL 6.2898 mL
    15 mM 0.1677 mL 0.8386 mL 1.6773 mL 4.1932 mL
    20 mM 0.1258 mL 0.6290 mL 1.2580 mL 3.1449 mL
    25 mM 0.1006 mL 0.5032 mL 1.0064 mL 2.5159 mL
    30 mM 0.0839 mL 0.4193 mL 0.8386 mL 2.0966 mL
    40 mM 0.0629 mL 0.3145 mL 0.6290 mL 1.5724 mL
    50 mM 0.0503 mL 0.2516 mL 0.5032 mL 1.2580 mL
    60 mM 0.0419 mL 0.2097 mL 0.4193 mL 1.0483 mL
    80 mM 0.0314 mL 0.1572 mL 0.3145 mL 0.7862 mL
    100 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.6290 mL
    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-443654552325-16-3A443654A 443654AktPKBProtein kinase BInhibitorinhibitorinhibit

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