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AG 490(JAK/ EGFR Inhibitor),>99%
【英文同義名】:Tyrphostin B42;AG 490; AG-490
【中文同義名】:
訂購信息:(*,常備現(xiàn)貨)
品 牌 | 產(chǎn)品名稱 | 產(chǎn)品貨號 | 規(guī) 格 | 目錄價(元) |
Gene Operation | AG 490 | IJS1002-0010MG | 10 mg | ¥2,019.00 |
IJS1002-0025MG | 25 mg | ¥3,629.00 | ||
IJS1002-0050MG | 50 mg | ¥5,449.00 |
產(chǎn)品描述
AG 490是細胞通透性的,可逆的,強效酪氨酸激酶抑制劑,研究中主要作為EGFR(IC50 = 0.1μM), JAK(JAK-2, JAK3/STAT, JAK3/AP-1, 和JAK3/MAPK)激酶抑制劑,并阻斷JAK3自磷酸化[1][2]。AG 490也會抑制EGF受體自磷酸化,其IC50 為100 nM,并抑制DNA合成和細胞生長[3]。通過誘導(dǎo)細胞凋亡,AG 490選擇性阻斷體內(nèi)外白血病細胞生長,但對正常造血作用不存在有害作用[4]。另外,AG 490抑制STAT-3 DNA結(jié)合的活化,及IL-2誘導(dǎo)的蕈樣肉芽腫(MF)腫瘤細胞的生長[5]。
靶點
Targets | EGFR |
|
IC50 | 0.1 μM[1] |
|
化學(xué)特性
Cas No.: 133550-30-8 | 分子量: 294.30 |
分子式: C17H14N2O3 | 純度: >99% |
同義名: Tyrphostin B42;AG 490; AG-490 | |
化學(xué)名: (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide | |
外觀: 黃色固體 | |
溶解: Soluble in DMSO(10 mg/ml ) or ethanol(5 mg/ml). Protect from light . | |
保存:Store powder at -20 ºC for the stability of three years. |
結(jié)構(gòu)式
參考文獻
[1] Gazit A,at el. Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem. 34(6):1896-907(1991).
[2] De Vos J, at el. JAK2 tyrosine kinase inhibitor tyrphostin AG490 downregulates the mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STAT) pathways and induces apoptosis in myeloma cells.Br J Haematol.109(4):823-8(2000).
[3] Kirken RA, at el.Tyrphostin AG-490 inhibits cytokine-mediated JAK3/STAT5a/b signal transduction and cellular proliferation of antigen-activated human T cells. J Leukoc Biol. 65(6):891-9(1999).
[4] Gonçalves S, at el.Tyrphostins as potential therapeutic agents for acute kidney injury. Curr Med Chem. 17(10):974-86(2010).
[5] Meydan N, at el.Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor. Nature. 379(6566):645-8(1996).