酪氨酸磷酸化抑制剂 AG 825

酪氨酸磷酸化抑制剂 AG 825用途

AG-825 是一种选择性、ATP竞争性,抑制酪氨酸磷酸化的 ErbB2 抑制剂,其 IC50 值为 0.35 μM。AG-825 具有抗癌活性。AG825 能明显加速人中性粒细胞的凋亡。AG-825 是一种潜在的克服锰诱导的神经毒性或阿尔茨海默病发展的药物。

酪氨酸磷酸化抑制剂 AG 825名称

[ CAS 号 ]:
149092-50-2

[ 中文名 ]:
5-[(苯并噻唑-2-基)硫甲基]-4-羟基-3-甲氧基亚苄基氰基乙酰胺

[ 英文名 ]:
AG-825

[中文别名 ]:

酪氨酸磷酸化抑制剂 AG825

[英文别名 ]:

TYRPHOSTIN C15

酪氨酸磷酸化抑制剂 AG 825生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> JAK/STAT信号通路 >> EGFR

信号通路 >> 蛋白酪氨酸激酶 >> EGFR

[ 靶点 ]

ErbB2:0.35 μM (IC50)

EGFR:19 μM (IC50)

[参考文献]

[1]. Wolfson E, et al. Nucleolin and ErbB2 inhibition reduces tumorigenicity of ErbB2-positive breast cancer. Cell Death Dis. 2018 Jan 19;9(2):47.

[2]. Gazit A, et al. Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins. J Med Chem. 1993 Nov 12;36(23):3556-64.

[3]. He H, et al. Signal therapy for RAS-induced cancers in combination of AG 879 and PP1, specific inhibitors for ErbB2 and Src family kinases, that block PAK activation. Cancer J. 2001 May-Jun;7(3):191-202.

[4]. Rahman A, et al. Inhibition of ErbB kinase signalling promotes resolution of neutrophilic inflammation. Elife. 2019 Oct 15;8. pii: e50990.

[5]. Ling J, et al. Identifying key genes, pathways and screening therapeutic agents for manganese-induced Alzheimer disease using bioinformatics analysis. Medicine (Baltimore). 2018 Jun;97(22):e10775.

酪氨酸磷酸化抑制剂 AG 825物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
689.3±65.0 °C at 760 mmHg

[ 分子式 ]:
C₁₉H₁₅N₃O₃S₂

[ 分子量 ]:
397.471

[ 闪点 ]:
370.7±34.3 °C

[ 精确质量 ]:
397.055481

[ PSA ]:
162.77000

[ LogP ]:
2.89

[ 外观性状 ]:
黄色固体

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.733

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
DMSO: soluble

酪氨酸磷酸化抑制剂 AG 825MSDS

详细MSDS(安全技术说明书)

酪氨酸磷酸化抑制剂 AG 825安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
22-24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

酪氨酸磷酸化抑制剂 AG 825文献

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