AG 490

AG 490CAS号: 133550-30-8分子式: C17H14N2O3分子量: 294.3描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vivo(体内研究)参考文献

产品描述
描述

AG-490 (Tyrphostin B42)是一种EGFR抑制剂,在无细胞试验中IC50为0.1μM,作用于EGFR比作用于ErbB2选择性高135倍,对JAK2也有抑制作用,对Lck,Lyn,Btk,Syk和Src没有抑制活性。

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
AG 490; Tyrphostin AG 490; AG490; Zinc02557947;AG-490 (Tyrphostin B42)
外观
yellow solid
可溶性/溶解性
DMSO:58 mg/mL (197.07 mM)

Ethanol:6 mg/mL (20.38 mM)

生物活性
靶点
EGFR
In vivo(体内研究)
AG490 significantly inhibits the development of type 1 diabetes (T1D) (p = 0.02, p = 0.005; at two different time points). Monotherapy of newly diagnosed diabetic NOD mice with AG490 (1 mg/mouse) markedly results in disease remission in treated animals (n=23) in comparision to the JPolute inability (0%; 0/10, p=0.003, Log-rank test) of DMSO and sustained eugluycemia is maintained for several months following drug withdrawal. AG490 (1-10 µg) significantly attenuates ʎ-carrageenan-induced thermal hyperalgesia in a dose-dependent manner. AG490 also reduces mechanical hyperalgesia.
参考文献
参考文献
[1] Gazit A, et al. J Med Chem, 1991, 34(6), 1896-1907.
[2] Meydan N, et al. Nature, 1996, 379(6566), 645-648.
[3] Nielsen M, et al. Proc Natl Acad Sci U S A, 1997, 94(13), 6764-6769.
[4] Kirken RA, et al. J Leukoc Biol, 1999, 65(6), 891-899.
[5] Sun X, et al. Blood, 2001, 97(7), 2008-2015.
[6] Burdelya L, et al. Mol Cancer Ther, 2002, 1(11), 893-899.
[7] Samanta AK, et al. Cancer Res, 2006, 66(13), 6468-6472.
[8] Abe M, et al. Int Immunopharmacol, 2009, 9(7-8), 870-877.

分子结构图

AG 490