FPA-124

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

FPA-124  纯度: ≥95.0%

FPA-124,一种细胞通透性铜配合物,是选择性的 Akt 抑制剂,IC50 为 0.1 μM ,与 Akt 的蛋白同源性 (PH) 域和激酶结构域相互作用。FPA-124 诱导细胞凋亡 (apoptosis)。

FPA-124

FPA-124 Chemical Structure

CAS No. : 902779-59-3

规格 价格 是否有货 数量
5 mg ¥4500 In-stock
10 mg ¥7500 In-stock
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100 mg   询价  

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FPA-124 相关产品

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生物活性

FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis[1][2].

体外研究
(In Vitro)

FPA-124 exhibits dose-dependent growth inhibitory effects with IC50s of 7, 10, 34, and 55 μM in BT20, PC-3, COLO 357 and BxPC-3 cancer cell lines, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

FPA-124 exhibits PKB (Akt protein) inhibitory activities and causes NF-κB inactivation in a well-established orthotopic pancreatic tumor model using COLO 357 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

381.73

Formula

C11H10Cl2CuN3O2S2-

CAS 号

902779-59-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (13.10 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6197 mL 13.0983 mL 26.1965 mL
5 mM 0.5239 mL 2.6197 mL 5.2393 mL
10 mM 0.2620 mL 1.3098 mL 2.6197 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: ≥ 0.67 mg/mL (1.76 mM); Clear solution

    此方案可获得 ≥ 0.67 mg/mL (1.76 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 6.7 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: 0.67 mg/mL (1.76 mM); Suspended solution; Need ultrasonic

    此方案可获得 0.67 mg/mL (1.76 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 6.7 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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Barve V, et al. Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells. J Med Chem. 2006 Jun 29;49(13):3800-8.

    [2]. Biscetti F, et al. Pioglitazone enhances collateral blood flow in ischemic hindlimb of diabetic mice through an Akt-dependent VEGF-mediated mechanism, regardless of PPARgamma stimulation. Cardiovasc Diabetol. 2009 Sep 8;8:49.

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