2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Akt Apoptosis
  4. PI3K/AKT-IN-1

PI3K/AKT-IN-1 是一种有效的 PI3K/AKT 双重抑制剂 (PI3Kγ、PI3Kδ 和 AKT 的 IC50分别为 6.99 μM、4.01 μM 和 3.36 μM)。PI3K/AKT-IN-1 具有抗癌活性，其作用机制是抑制 PI3K/AKT 通路，诱导 caspase 3 依赖性凋亡 (apoptosis)。

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PI3K/AKT-IN-1 Chemical Structure

PI3K/AKT-IN-1 Chemical Structure

CAS No. : 3033069-84-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2560
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1 mg ￥1136
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5 mg ￥2500
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10 mg ￥4200
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Customer Review

PI3K/AKT-IN-1 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis[1].

IC50 & Target[1]

PI3Kγ

6.99 μM (IC50)

PI3Kδ

4.01 μM (IC50)

体外研究
(In Vitro)

PI3K/AKT-IN-1 (compound 7f) (0.04-100 µM; 48 hours) has high cytotoxic activity on both cell lines with better activity on leukaemia cell line (K562 IC50=2.62 µM) than on the breast cancer cell line (MCF-7 IC50=3.22 µM)[1].
PI3K/AKT-IN-1 (2.62 µM) can promote S-phase cell cycle arrest and apoptosis induction in K562 cells[1].
PI3K/AKT-IN-1 (2.62 µM; 48 hours) causes an increase in the percentage of Annexin-V positive apoptotic cells both in the early and late stage[1].
PI3K/AKT-IN-1 (2.62 µM; 48 hours) markedly reduces the expression of PI3K, AKT, Cyclin D1 and NF-κB[1].

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

PI3K/AKT-IN-1 相关抗体:

Cell Cytotoxicity Assay

Cell Line: MCF-7 and K562 cells[1]
Concentration: 0.04-100 µM
Incubation Time: 48 hours
Result: Demonstrated high cytotoxic activity on both cell lines with better activity on leukaemia cell line (K562 IC50=2.62 µM) than on the breast cancer cell line (MCF-7 IC50=3.22 µM).

Cell Cycle Analysis

Cell Line: K562 cells[1]
Concentration: 2.62 µM
Incubation Time:
Result: Promoted S-phase cell cycle arrest and apoptosis induction.

Apoptosis Analysis

Cell Line: K562 cells[1]
Concentration: 2.62 µM
Incubation Time: 48 hours
Result: Caused an increase in the percentage of Annexin-V positive apoptotic cells both in the early and late stage.

Western Blot Analysis

Cell Line: K562 cells[1]
Concentration: 2.62 µM
Incubation Time: 48 hours
Result: Markedly reduced the expression of PI3K, p-PI3K, AKT, p-AKT, Cyclin D1 and NF-κB.
体内研究
(In Vivo)

PI3K/AKT-IN-1 (2000 mg/kg; p.o.; single) is non-toxic and is well tolerated by experimental animals[1].

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

Animal Model: Female rats (180-200g)[1]
Dosage: 2000 mg/kg
Administration: p.o.; single
Result: The median lethal dose (LD50) was greater than the test dose (2000 mg/kg).
分子量

465.52

Formula

C23H23N5O4S
CAS 号
性状

固体

颜色

Off-white to light yellow

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
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (107.41 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 2.1481 mL 10.7407 mL 21.4814 mL
5 mM 0.4296 mL 2.1481 mL 4.2963 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。-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。

  • 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
纯度 & 产品资料
参考文献

PI3K/AKT-IN-1 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。-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 1 mM 2.1481 mL 10.7407 mL 21.4814 mL 53.7034 mL
5 mM 0.4296 mL 2.1481 mL 4.2963 mL 10.7407 mL
10 mM 0.2148 mL 1.0741 mL 2.1481 mL 5.3703 mL
15 mM 0.1432 mL 0.7160 mL 1.4321 mL 3.5802 mL
20 mM 0.1074 mL 0.5370 mL 1.0741 mL 2.6852 mL
25 mM 0.0859 mL 0.4296 mL 0.8593 mL 2.1481 mL
30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7901 mL
40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3426 mL
50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0741 mL
60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8951 mL
80 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.6713 mL
100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5370 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:

PI3K/AKT-IN-13033069-84-7PI3KAktApoptosisPhosphoinositide 3-kinasePKBProtein kinase BPyrimidine-5-carbonitrileleukaemiaBreast cancerLeukaemia K562MCF-7PI3K/AKT pathwayDual inhibitorInhibitorinhibitorinhibit

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