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

A-443654 

目录号: HY-10425 纯度: 98.50%
产品使用指南

A-443654 是一种有效的 pan-Akt 抑制剂,以同等效力抑制 Akt1Akt2,和 Akt3Ki 值均为 160 pM。

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A-443654 Chemical Structure

A-443654 Chemical Structure

CAS No. : 552325-16-3

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3148
In-stock
1 mg ¥1200
In-stock
5 mg ¥3600
In-stock
10 mg ¥6500
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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Top Publications Citing Use of Products

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

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

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

    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.

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

    查看 Akt 亚型特异性产品:

    • 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)

    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.

    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
    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 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : ≥ 100 mg/mL (251.59 mM)

    * "≥" 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
    10 mM 0.2516 mL 1.2580 mL 2.5159 mL
    *

    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。-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。

    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

    • 1.

      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); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (6.29 mM,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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 2.

      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); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (6.29 mM,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。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (6.29 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      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玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    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
    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    A-443654
    目录号:
    HY-10425
    需求量: