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Tyrphostin AG 879

Tyrphostin AG 879用途

AG879是酪氨酸激酶的抑制剂,能够抑制TrKA的磷酸化,但不能抑制TrKB 和TrKC,也是高选择性的ErbB2激酶抑制剂。

Tyrphostin AG 879名称

[ CAS 号 ]:
148741-30-4

[ 中文名 ]:
Tyrphostin AG 879

[ 英文名 ]:
Tyrphostin AG 879

[英文别名 ]:

AG 879
BMK1-D4
Lopac-T-2067
Tyrphostin AG 879

Tyrphostin AG 879生物活性

[ 描述 ]:

AG879是酪氨酸激酶的抑制剂,能够抑制TrKA的磷酸化,但不能抑制TrKB 和TrKC,也是高选择性的ErbB2激酶抑制剂。

[ 相关类别 ]:

信号通路 >> 蛋白酪氨酸激酶 >> Trk Receptor

研究领域 >> 癌症

[参考文献]

[1]. Rende M et al. Role of nerve growth factor and its receptors in non-nervous cancer growth: efficacy of a tyrosine kinase inhibitor (AG879) and neutralizing antibodies antityrosine kinase receptor A and antinerve growth factor: an in-vitro and in-vivo study. Anticancer Drugs. 2006 Sep;17(8):929-41.

[2]. Zhou Y et al. Blockade of EGFR and ErbB2 by the novel dual EGFR and ErbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma GEO cells to apoptosis. Cancer Res. 2006 Jan 1;66(1):404-11.

[3]. Ting AK et al. Neuregulin 1 promotes excitatory synapse development and function in GABAergic interneurons. J Neurosci. 2011 Jan 5;31(1):15-25.

[相关活性小分子]

Tyrphostin AG 879物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
432.7±55.0 °C at 760 mmHg

[ 熔点 ]:
232 °C

[ 分子式 ]:
C₁₈H₂₄N₂OS

[ 分子量 ]:
316.461

[ 闪点 ]:
215.5±31.5 °C

[ 精确质量 ]:
316.160919

[ PSA ]:
102.13000

[ LogP ]:
4.76

[ 外观性状 ]:
固体;Light yellow to Yellow to Orange powder to crystal

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.600

[ 储存条件 ]:
Store at -20°C

[ 水溶解性 ]:
DMSO: at 26 mg/mlsoluble

Tyrphostin AG 879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

[ 海关编码 ]:
2930909090

Tyrphostin AG 879海关

[ 海关编码 ]: 2930909090

[ 中文概述 ]:
2930909090. 其他有机硫化合物. 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:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2930909090. other organo-sulphur compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

Tyrphostin AG 879文献

Initiation of testicular tubulogenesis is controlled by neurotrophic tyrosine receptor kinases in a three-dimensional Sertoli cell aggregation assay.

Reproduction 136 , 459-69, (2008)

The first morphological sign of testicular differentiation is the formation of testis cords. Prior to cord formation, newly specified Sertoli cells establish adhesive junctions, and condensation of so...

Comparison of delphinidin, quercetin and (-)-epigallocatechin-3-gallate as inhibitors of the EGFR and the ErbB2 receptor phosphorylation.

Mol. Nutr. Food. Res. 52(7) , 815-22, (2008)

In the present study, delphinidin was found to suppress the phosphorylation of the epidermal growth factor receptor (EGFR) within human tumour cells (human colon carcinoma cell line (HT29), human vulv...

The Tyr-kinase inhibitor AG879, that blocks the ETK-PAK1 interaction, suppresses the RAS-induced PAK1 activation and malignant transformation.

Cancer Biol. Ther. 3(1) , 96-101, (2004)

AG 879 has been widely used as a Tyr kinase inhibitor specific for ErbB2 and FLK-1, a VEGF receptor. The IC(50) for both ErbB2 and FLK-1 is around 1 microM. AG 879, in combination of PP1 (an inhibitor...

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