2. PI3K/Akt/mTOR
  3. Akt
  4. PF-AKT400

PF-AKT400  (Synonyms: AKT protein kinase inhibitor)

目录号: HY-10721 纯度: ≥98.0%
COA 产品使用指南

摩尔计算器

PF-AKT400 是一种有效的, ATP 竞争性的选择性 Akt 抑制剂，对 PKBα (IC50=0.5 nM) 的选择性比 PKA (IC50=450 nM) 高 900 倍。

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PF-AKT400 Chemical Structure

PF-AKT400 Chemical Structure

CAS No. : 1004990-28-6

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10 mg ￥4200
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Customer Review

Other Forms of PF-AKT400:

PF-AKT400 相关抗体

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).

IC50 & Target[1]

PKBα

0.5 nM (IC50)

PKA

450 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
U-87MG ATCC IC50
0.31 μM
Compound: 42
Inhibition of AKT1-mediated GSK3alpha phosphorylation in human U87 cells after 1 hr by ELISA
Inhibition of AKT1-mediated GSK3alpha phosphorylation in human U87 cells after 1 hr by ELISA
[PMID: 20481595]
体外研究
(In Vitro)

PF-AKT400 (Compound 42) provides significantly enhanced selectivity for Akt relative to earlier leads such as spiroindoline 2. Free IC50 and EC50 values are estimated for phospho-S6 reduction (110 nM) and Akt hyperphosphorylation (216 nM), respectively. These values corresponded well to the cellular IC50 for PF-AKT400 in U87 cells measuring p-GSK-3α (310 nM)[2].

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

PF-AKT400 相关抗体:
体内研究
(In Vivo)

PF-AKT400 is subsequently evaluated for modulation of Akt in tumors and in multiple in vivo mouse models of antitumor efficacy. It is active in a PC3 prostate carcinoma xenograft experiment, with 75% TGI observed at 100 mg/kg b.i.d. dosing for 10 days. In a colorectal carcinoma (Colo205) xenograft study, PF-AKT400 produces 60% TGI at 150 mg/kg b.i.d. after 10 days. Most intriguingly, in combination with Rapamycin (10 mg/kg, ip), 75 mg/kg b.i.d. (10 days) of PF-AKT400 results in 98% TGI in an additional PC3 prostate carcinoma xenograft study compared to 56% TGI and 66% TGI with PF-AKT400 and Rapamycin as single agents. To define the in vivo potency of PF-AKT400 (Compound 42) in the PC3 xenograft model, oral administration of 25, 75, and 100 mg/kg PF-AKT400 is performed with blood and tumor sampling over time. Immunoblot analysis of detergent-soluble extracts derived from PC3 tumors shows a significant reduction of S6 phosphorylation, and hyperphosphorylation of Akt upon treatment at doses that produced significant tumor growth inhibition. Plasma drug concentrations peak rapidly after oral administration of doses between 25-100 mg/kg (Tmax=0.5 h). Peak PD responses of phospho-S6 and phospho-Akt are observed at approximately 2-4h and 1h post-administration of PF-AKT400, respectively. The time-course of PD marker response is well described by a PK/PD model at doses that ranged from no efficacy (25 mg/kg) to maximal efficacy (100 mg/kg)[2].

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

400.43

Formula

C20H22F2N6O
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 (249.73 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 2.4973 mL 12.4866 mL 24.9732 mL
5 mM 0.4995 mL 2.4973 mL 4.9946 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 (6.24 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 (6.24 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
Kinase Assay
[2]

A fluorescence polarization IMAP type assay is used. An amount of 15 μL of diluted PF-AKT400 (Compound 42) in DMSO is mixed with 60 μL of reaction buffer (10 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.01% Triton-X100, 1 mM DTT). Then 5 μL of the compound/buffer mixture, 10 μL of a solution containing 4 μM ATP and 40 nM fluorescent-labeled Crosstide (Tamara-labeled GRPRTSSFAEG peptide), and 5 μL of Akt1 protein (lacking the pleckstrin homology (PH) domain, containing an Asp at position 473, and prephosphorylated at Thr 308) in reaction buffer are combined. After a 90 min incubation, IMAP beads are added and plates are read (lamp filter, 544 nm; emission filter, 615 nm). The same procedure can be applied to full length Akt1 to provide similar results. All IC50 values are the geometric mean of at least n=2 determinations[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
Studies to describe the PK/PD relationship for PF-AKT400 are performed in male SCID/Beige mice bearing subcutaneous PC3 prostate carcinoma xenografts. Once tumors reach about ~300mm3 in size, PF-AKT400 is formulated in 0.5% methylcellulose vehicle and administered orally to 3 mice per dose group. Plasma and tumors are harvested over time, tumor lysates prepared, and the levels of phospho S6 reduction and phospho Akt induction are evaluated by immunoblot.

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

PF-AKT400 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 2.4973 mL 12.4866 mL 24.9732 mL 62.4329 mL
5 mM 0.4995 mL 2.4973 mL 4.9946 mL 12.4866 mL
10 mM 0.2497 mL 1.2487 mL 2.4973 mL 6.2433 mL
15 mM 0.1665 mL 0.8324 mL 1.6649 mL 4.1622 mL
20 mM 0.1249 mL 0.6243 mL 1.2487 mL 3.1216 mL
25 mM 0.0999 mL 0.4995 mL 0.9989 mL 2.4973 mL
30 mM 0.0832 mL 0.4162 mL 0.8324 mL 2.0811 mL
40 mM 0.0624 mL 0.3122 mL 0.6243 mL 1.5608 mL
50 mM 0.0499 mL 0.2497 mL 0.4995 mL 1.2487 mL
60 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0405 mL
80 mM 0.0312 mL 0.1561 mL 0.3122 mL 0.7804 mL
100 mM 0.0250 mL 0.1249 mL 0.2497 mL 0.6243 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:

PF-AKT4001004990-28-6AKT protein kinase inhibitorAktPKBProtein kinase BInhibitorinhibitorinhibit

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