PI3K/AKT-IN-1|西域试剂

PI3K/AKT-IN-1,99.62%

产品编号：Bellancom-144806| 分子式：C₂₃H₂₃N₅O₄S| 分子量：465.52

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货号	价格	库存与货期
Bellancom-144806	￥2500.00	杭州北京（现货）
Bellancom-144806	￥4200.00	杭州北京（现货）
Bellancom-144806	￥9200.00	杭州北京（现货）
Bellancom-144806	￥15000.00	杭州北京（现货）

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PI3K/AKT-IN-1

产品介绍

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)。

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.

体外研究

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).
PI3K/AKT-IN-1 (2.62 µM) can promote S-phase cell cycle arrest and apoptosis induction in K562 cells.
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.
PI3K/AKT-IN-1 (2.62 µM; 48 hours) markedly reduces the expression of PI3K, AKT, Cyclin D1 and NF-κB.

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

Cell Cytotoxicity Assay

Cell Line:	MCF-7 and K562 cells
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
Concentration:	2.62 µM
Incubation Time:
Result:	Promoted S-phase cell cycle arrest and apoptosis induction.

Apoptosis Analysis

Cell Line:	K562 cells
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
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.

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

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

体内研究

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

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

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

体内研究

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

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

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (107.41 mM; Need ultrasonic)

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
10 mM	0.2148 mL	1.0741 mL	2.1481 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式