658401
AG 490
A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC₅₀ = 100 nM).
别名:
AG 490, α-Cyano-(3,4-dihydroxy)-N-benzylcinnamide, Tyrphostin B42, ( E)- N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI, α-Cyano-(3,4-dihydroxy)-N-benzylcinnamide, Tyrphostin B42, (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI
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About This Item
推荐产品
品質等級
化驗
≥98% (HPLC)
形狀
solid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
yellow
溶解度
DMSO: 100 mg/mL
運輸包裝
ambient
儲存溫度
−20°C
InChI
1S/C17H14N2O3/c18-10-14(8-13-6-7-15(20)16(21)9-13)17(22)19-11-12-4-2-1-3-5-12/h1-9,20-21H,11H2,(H,19,22)/b14-8+
InChI 密鑰
TUCIOBMMDDOEMM-RIYZIHGNSA-N
一般說明
A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM). Inhibition of JAK2 by AG 490 selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal hematopoiesis. Inhibits the constitutive activation of STAT-3 DNA binding and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3. A 100 mM (5 mg/170 µl) solution of AG490 (Cat. No. 658411) in DMSO is also available.
A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM). Jak family tyrosine kinase inhibitor. Inhibition of Jak2 by AG 490 selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal haematopoiesis. Inhibits the constitutive activation of STAT-3 and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3. Also reported to inhibit guanylyl cyclase.
生化／生理作用
Cell permeable: yes
Primary Target
epidermal growth factor receptor kinase autophosphorylation
epidermal growth factor receptor kinase autophosphorylation
Product does not compete with ATP.
Reversible: yes
Target IC50: 100 nM against epidermal growth factor receptor kinase autophosphorylation
警告
Toxicity: Standard Handling (A)
重構
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
其他說明
Jaleel, M., et al. 2004. Biochemistry43, 8247.
Eriksen, K.W., et al. 2001. Leukemia15, 787.
Kirken, R.A., et al. 1999. Leukoc. Biol.65, 891.
Nielsen, M., et al. 1997. Proc. Natl. Acad. Sci. USA 94, 6764.
Meydan, N., et al. 1996. Nature 379, 645.
Gazit, A., et al. 1991. J. Med. Chem.34, 1896.
Levitzki, A. 1990. Biochem. Pharmacol.40, 913.
Eriksen, K.W., et al. 2001. Leukemia15, 787.
Kirken, R.A., et al. 1999. Leukoc. Biol.65, 891.
Nielsen, M., et al. 1997. Proc. Natl. Acad. Sci. USA 94, 6764.
Meydan, N., et al. 1996. Nature 379, 645.
Gazit, A., et al. 1991. J. Med. Chem.34, 1896.
Levitzki, A. 1990. Biochem. Pharmacol.40, 913.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
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