Alsterpaullone - CAS:237430-03-4

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Alsterpaullone (Synonyms:9-Nitropaullone; NSC 705701)

目录号 : KM7391 CAS No. : 237430-03-4 纯度 : ≥98%

Data Sheet SDS 产品使用指南

Alsterpaullone (9-Nitropaullone) 是一种高效的 CDK 抑制剂，作用于 CDK1/cyclin B、CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p35 的 IC₅₀ 值分别为 35 nM、15 nM、200 nM 和 40 nM。Alsterpaullone 是 ATP 竞争性的 GSK-3alpha/GSK-3beta 抑制剂，且作用的 IC₅₀ 值都为 4 nM。Alsterpaullone 具有抗肿瘤活性，有用于神经退行性和增生性疾病研究的潜力。Alsterpaullon 诱导白血病细胞凋亡 (apoptosis)。

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50mg	询价	In-stock

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生物活性

Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC₅₀s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC₅₀s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line.

IC₅₀&Target

Cdk1/cyclin B

35 nM (IC₅₀)

cdk2/cyclin A

15 nM (IC₅₀)

CDK2/Cyc E

200 nM (IC₅₀)

CDK5/p35

40 nM (IC₅₀)

GSK-3α

4 (IC₅₀)

GSK-3β

4 nM (IC₅₀)

体外研究

Alsterpaullone (0.3, 1, 3 μM; 8 hours) induces apoptosis in leukemia cell line.
Alsterpaullone (5, 10, 15, 20, 25, 30 μM; 48 and 72 hours) inhibits the growth of HeLa cells in dose-and time-dependent manner. Treatment with Alsterpaullone causes a time-dependent inhibition of cell growth too.
Alsterpaullone (20 μM) induces cell death depending on caspase activity.

Cell Viability Assay

Cell Line:	HeLa cells
Concentration:	5, 10, 15, 20, 25, 30 μM
Incubation Time:	48 and 72 hours
Result:	The growth of HeLa cells was inhibited in a dose-dependent manner for 48 h and 72 h ranging from 0 to 30 μM.

Apoptosis Analysis

Cell Line:	Jurkat cell line
Concentration:	0.3, 1, 3 μM
Incubation Time:	8 hours
Result:	Induced dose-dependent apoptosis. 1 μM was sufficient to cause apoptosis, 3 μM demonstrated maximal apoptotic effects.

Western Blot Analysis

Cell Line:	HeLa cells
Concentration:	2, 4, 6, 12, 24 hours
Incubation Time:	8 hours
Result:	The cleavage of PARP started at 4 h, while the activation of caspase-3 occurred at 2 h.

体内研究

Alsterpaullone (30 mg/kg, s.c., daily for 2 weeks) reduces tumor growth and increases survival in medulloblastoma xenografts.

Animal Model:	5-6 week old athymic nude mice
Dosage:	30 mg/kg
Administration:	Subcutaneous injections, daily for 2 weeks
Result:	Antitumor effect in Group 3 medulloblastomas.

分子式

C₁₆H₁₁N₃O₃

分子量

293.28

CAS号

237430-03-4

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

纯度： ≥98%

Data Sheet

SDS

产品使用指南

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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动物实验计算换算器