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抑制剂/激活剂

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凋亡与自噬

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AG-490 Tyrphostin AG490; Tyrphostin B42

AG-490是一种EGFR抑制剂，在无细胞试验中IC50为0.1 μM，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。

货号：
TK0117
规格：

5mg

10mg

25mg

50mg
价格：
￥0.00

产品参数

CAS No.	133550-30-8
生物活性	AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
分子式	C17H14N2O3
分子量	294.3
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : ≥ 50 mg/mL (169.89 mM)
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 ʎ-carrageenan-induced thermal hyperalgesia in a dose-dependent manner. AG490 also reduces mechanical hyperalgesia.
体外研究	AG490 inhibits the activation of Stat-3 by selectively blocking JAK2. AG490 is used to selectively inhibit JAK/Stat-3 activation. At a dose of 10 μM, Stat-3 phosphorylation is decreased by >95% and cell viability is maintained. AG490 at a dose of 10 μM results in >95% decrease in pStat-3 in EGF-stimulated A431 cells with no effect on Stat-3 mass. AG-490 is a potent inhibitor of the JAK3/STAT, JAK3/AP-1, and JAK3/MAPK pathways and their cellular consequences. AG-490 abolishes IL-2-inducible [H]thymidine incorporation in a dose-dependent manner, displaying an IC50 of 25 μM. AG-490 potently inhibits IL-2-mediated proliferation in T cells, results distinct from previous studies that showed this agent induced apoptosis in ALL cells while exerting apparently no effects on the growth of mitogen-stimulated normal T cells.
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纯度及产品资料	98%

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