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(3,4-二羟基苄基)丙二腈

(3,4-二羟基苄基)丙二腈用途

Tyrphostin 23 (Tyrphostin A23) 是 EGFR 的抑制剂,IC50 值为35 μM。

(3,4-二羟基苄基)丙二腈名称

[ CAS 号 ]:
118409-57-7

[ 中文名 ]:
(3,4-二羟基苄基)丙二腈

[ 英文名 ]:
AG 18

[中文别名 ]:

[英文别名 ]:

(3,4-dihydroxybenzylidene)propanedinitrile
MFCD00133899
(3,4-Dihydroxybenzylidene)malononitrile RG-50810
(3,4-Dihydroxybenzylidene)malononitrile
AG 18
AG-18

(3,4-二羟基苄基)丙二腈生物活性

[ 描述 ]:

Tyrphostin 23 (Tyrphostin A23) 是 EGFR 的抑制剂,IC50 值为35 μM。

[ 相关类别 ]:

研究领域 >> 癌症

[ 靶点 ]

EGFR:35 μM (IC50, Cell Assay)

EGFR:11 μM (Ki)

[体外研究]

10μM的tyrphostin 23可显着抑制由1 nM和1μM生长素释放肽引起的细胞增殖[2]。 Tyrphostin 23(T23)是一种众所周知的蛋白酪氨酸激酶抑制剂,被认为是潜在的抗癌药物。据报道,T23急剧刺激原代培养的星形胶质细胞中的糖酵解通量。 Tyrphostin 23刺激培养的星形胶质细胞中的糖酵解通量。 Tyrphostin 23暴露可加速脑星形胶质细胞的线粒体代谢[3]。

[参考文献]

[1]. Gazit A, et al. Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem. 1989 Oct;32(10):2344-52.

[2]. Nanzer AM, et al. Ghrelin exerts a proliferative effect on a rat pituitary somatotroph cell line via the mitogen-activated protein kinase pathway. Eur J Endocrinol. 2004 Aug;151(2):233-40.

[3]. Hohnholt MC, et al. The tricarboxylic acid cycle activity in cultured primary astrocytes is strongly accelerated by the protein tyrosine kinase inhibitor tyrphostin 23. Neurochem Int. 2017 Jan;102:13-21.

[相关活性小分子]

(3,4-二羟基苄基)丙二腈物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
421.1±45.0 °C at 760 mmHg

[ 熔点 ]:
225ºC

[ 分子式 ]:
C₁₀H₆N₂O₂

[ 分子量 ]:
186.167

[ 闪点 ]:
208.5±28.7 °C

[ 精确质量 ]:
186.042923

[ PSA ]:
88.04000

[ LogP ]:
0.99

[ 外观性状 ]:
黄色-黄褐色的固体

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.697

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
Soluble in DMSO, ethanol, or DMF

(3,4-二羟基苄基)丙二腈MSDS

详细MSDS(安全技术说明书)

(3,4-二羟基苄基)丙二腈安全信息

[ 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

(3,4-二羟基苄基)丙二腈合成路线

详细合成路线

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(3,4-二羟基苄基)丙二腈文献

Regulation of store-operated Ca2+ entry in pulmonary artery smooth muscle cells.

Cell Calcium 46(2) , 99-106, (2009)

Store-operated Ca2+ entry (SOCE) is an important mechanism for Ca2+ influx in smooth muscle cells; however the activation and regulation of this influx pathway are incompletely understood. In the pres...

Spatio-temporal cellular dynamics of the Arabidopsis flagellin receptor reveal activation status-dependent endosomal sorting.

Plant Cell 24(10) , 4205-19, (2012)

The activity of surface receptors is location specific, dependent upon the dynamic membrane trafficking network and receptor-mediated endocytosis (RME). Therefore, the spatio-temporal dynamics of RME ...

Swelling-activated K+ efflux and regulatory volume decrease efficiency in human bronchial epithelial cells.

J. Membr. Biol. 214(1) , 33-41, (2006)

This study describes the correlation between cell swelling-induced K+ efflux and volume regulation efficiency evaluated with agents known to modulate ion channel activity and/or intracellular signalin...

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