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抑制剂描述:

产品名称:AG 490

产品别名:见爱必信官网

英文别名:AG 490

靶点:EGFR

CAS:133550-30-8

纯度:>98%

外观:见爱必信官网

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.

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。

溶解性:DMSO:58 mg/mL (197.07 mM)
Ethanol:6 mg/mL (20.38 mM)

体外研究:

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 absolute 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 ?-carrageenan-induced thermal hyperalgesia in a dose-dependent manner. AG490 also reduces mechanical hyperalgesia.

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