Purvalanol A.

更新时间：2024-01-02 09:26:27

Purvalanol A.结构式	常用名	Purvalanol A.	英文名	Purvalanol A
	CAS号	212844-53-6	分子量	388.894
	密度	1.3±0.1 g/cm3	沸点	590.5±60.0 °C at 760 mmHg
	分子式	C₁₉H₂₅ClN₆O	熔点	N/A
	MSDS	中文版美版	闪点	310.9±32.9 °C

Purvalanol A.用途

Purvalanol A 是一种有效的 CDK 抑制剂,对 cdc2-cyclin B,cdc2-cyclin B,cdk2-cyclin E,cdk4-cyclin D1 和 cdk5-p35 的 IC50 值分别为 4,70,35,850 和 75 nM。

中文名	Purvalanol A.
英文名	purvalanol A
英文别名	更多

描述	Purvalanol A 是一种有效的 CDK 抑制剂,对 cdc2-cyclin B,cdc2-cyclin B,cdk2-cyclin E,cdk4-cyclin D1 和 cdk5-p35 的 IC50 值分别为 4,70,35,850 和 75 nM。
相关类别	信号通路 >> 自噬 >> 自噬研究领域 >> 癌症
靶点	cdc2-cyclin B:4 nM (IC50) cdk2-cyclin E:35 nM (IC50) cdk2-cyclin A:70 nM (IC50) cdk4-cyclin D1:850 nM (IC50) cdk5-p35:75 nM (IC50) erk1:9000 nM (IC50)
体外研究	Purvalanol A抑制cdc28(酿酒酵母)和erk1,IC50为80和9000 nM。 Purvalanol A显示出针对60个人肿瘤细胞系的NCI组的抑制活性,平均GI50为2μM;两种细胞系对purvalanol A的敏感性增加~20倍：GI12为76 nM的KM12结肠癌细胞系和NCI-H522非小细胞肺癌细胞系,GI50为347 nM [1] 。 Purvalanol A是CDK2的2.5倍强效抑制剂,但在低微摩尔范围内也有效抑制DYRK1A和许多其他蛋白激酶。 Purvalanol A抑制MKK1,MAPK2/ERK2,JNK/SAPK1c,IC50分别为80,26,84μM[2]。 Purvalanol A选择性地抑制细胞蛋白的磷酸化。 Purvalanol A可防止血清诱导的G1期进展过程中细胞周期蛋白D和E含量的增加。 Purvalanol A在无细胞条件下不抑制转录[3]。
参考文献	[1]. Gray NS, et al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8. [2]. Bain J, et al. The specificities of protein kinase inhibitors: an update. Biochem J. 2003 Apr 1;371(Pt 1):199-204. [3]. Villerbu N, et al. Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int J Cancer. 2002 Feb 20;97(6):761-9.

密度	1.3±0.1 g/cm3
沸点	590.5±60.0 °C at 760 mmHg
分子式	C₁₉H₂₅ClN₆O
分子量	388.894
闪点	310.9±32.9 °C
精确质量	388.177826
PSA	87.89000
LogP	2.77
外观性状	粉末
蒸汽压	0.0±1.7 mmHg at 25°C
折射率	1.654
储存条件	−20°C
水溶解性	methylene chloride: 50 mg/mL, clear, colorless

个人防护装备	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
危险品运输编码	NONH for all modes of transport
WGK德国	3
海关编码	2933990090

海关编码	2933990090
中文概述	2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素	品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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Purvalanol A

Purv