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AG 18

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Chemical Structure| 118409-57-7 同义名 : RG-50810;Tyrphostin A23;Tyrphostin AG-18;RG-50858;TX 825;Tyrphostin 23
CAS号 : 118409-57-7
货号 : A423886
分子式 : C10H6N2O2
纯度 : 99%+
分子量 : 186.167
MDL号 : MFCD00133899
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(564.01 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • EGFR/ErbB1

    EGFR, IC50:35 μM
描述 Tyrphostin 23 (AG 18) is an EGFR inhibitor with an IC50 and Kiof 35 and 11 μM, respectively[3]. Tyrphostins (structural analogs of tyrosine) are inhibitors of tyrosine kinases and function by binding to the active sites of the enzymes. Control tyrphostins, active as inhibitors of tyrosine kinase activity, but incapable of inhibiting the YXXPhi motif/mu2 interaction, did not inhibit endocytosis[4]. The stimulation of glycolytic flux by T23 (Tyrphostin 23) was reversible, completely abolished upon removal of the compound and not found in presence of other known inhibitors of endocytosis. T23-sensitive phosphorylation/dephosphorylation events are involved in the regulation of astrocytic glycolysis[5]. Tyrphostin A23 and A63 stimulate the cAMP-activated CFTR (cystic fibrosis transmembrane conductance regulator) Cl(-) channel via a PTK(an inhibitor of protein tyrosine kinase)-independent, structure-dependent mechanism[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01306305 Influenza Phase 4 Completed - Switzerland ... 展开 >> Covance Clinical Research Unit AG Allschwil, Switzerland, 4123 收起 <<
NCT02322437 Mental Disorders Not Applicable Completed - Switzerland ... 展开 >> Psychiatric Services Aargau AG Brugg, Aargau, Switzerland, 5201 收起 <<
NCT01306305 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.37mL

1.07mL

0.54mL

26.86mL

5.37mL

2.69mL

53.72mL

10.74mL

5.37mL
参考文献

[1]Nanzer AM, Khalaf S, 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.

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

[3]Gazit A, Yaish P, Gilon C, Levitzki A. Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem. 1989 Oct;32(10):2344-52

[4]Banbury DN, Oakley JD, Sessions RB, Banting G. Tyrphostin A23 inhibits internalization of the transferrin receptor by perturbing the interaction between tyrosine motifs and the medium chain subunit of the AP-2 adaptor complex. J Biol Chem. 2003 Apr 4;278(14):12022-8

[5]Blumrich EM, Kadam R, Dringen R. The Protein Tyrosine Kinase Inhibitor Tyrphostin 23 Strongly Accelerates Glycolytic Lactate Production in Cultured Primary Astrocytes. Neurochem Res. 2016 Oct;41(10):2607-2618

[6]Niisato N, Nishio K, Marunaka Y. Activation of CFTR Cl(-) channel by tyrphostins via a protein tyrosine kinase-independent pathway in forskolin-stimulated renal epithelial A6 cells. Life Sci. 2002 Jul 26;71(10):1199-207